BODIPY 503/512 is a lipophilic, amine-reactive fluorescent probe. It has been used to label oligonucleotide probes and primers for the quantitation of DNA and RNA by PCR and to monitor the uptake and trafficking of BODIPY-labeled proteins and other compounds within cells by fluorescence microscopy. BODIPY 503/512 has also been used to identify and sort adipocytes from mouse white and brown adipose tissue by flow cytometry. It displays excitation/emission maxima of 503/512 nm, respectively.

Z-LRGG-AMC TFA is a fluorogenic substrate for isopeptidase T. Upon enzymatic cleavage by isopeptidase T, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify isopeptidase T activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.

Sodium Ionophore VI is a sodium-selective ionophore that can be used in ion-selective electrodes to monitor sodium levels in aqueous solutions. It is selective for sodium over calcium, magnesium, lithium, ammonium, and potassium ions. Sodium ionophore VI has been used in electrodes to determine the levels of sodium ions in human urine and serum, as well as in X. laevis oocytes.

7,8-Dihydroneopterin is a pteridine with antioxidant activities. It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals and inhibits copper ion-induced oxidation of LDL. It also decreases thiobarbituric acid reactive substances (TBARS) produced by THP-1 cells cultured with LDL, and it inhibits necrosis induced by oxidized LDL (oxLDL).

Sulforhodamine 101 sulfonyl chloride is a fluorescent probe that binds to free amino groups and is a derivative of sulforhodamine 101. It displays excitation/emission maxima of 585/602 nm, respectively. Sulforhodamine 101 sulfonyl chloride has commonly been used as a fluorescent conjugate on antibodies or proteins for the detection of proteins via fluorescent microscopy and flow cytometry applications.

Cerebroside C is a fungal metabolite and glycosphingolipid that induces production of the phytoalexin momilactone A when applied to wounded rice leaves, indicating that cerebroside C is an elicitor of the hypersensitive response in rice. Cerebroside C increases germination rate and reduces germination time in wheat seeds in a concentration-dependent manner at 4°C. It also increases root length, fresh weight, and dry weight of wheat seedlings when used at a concentration of 20 μg/ml at 4°C, indicating increased chilling tolerance.

Pyrenophorol is a fungal metabolite that has been found in Alternaria and has diverse biological activities. It inhibits human topoisomerase II α when used at concentrations of 75 and 100 μM. It is active against S. cerevisiae (MIC = 4 μM) and M. violaceum. Pyrenophorol induces leaf necrosis and chlorophyll retention in wild oats when used at a concentration of 64 μM.

TPTZ is a colorimetric reagent commonly used in the detection of iron. TPTZ forms a complex with Fe(II) that can be quantified by colorimetric detection at 594 nm as a measure of iron concentration.

Resorufin β-D-Galactopyranoside is a fluorogenic substrate for β-galactosidase. Upon enzymatic cleavage by β-galactosidase, the fluorescent moiety resorufin is released and its fluorescence can be used to quantify β-galactosidase activity. Resorufin displays excitation/emission maxima of 570/580 nm, respectively.

3'-O-dephosphono-coenzyme A is an intermediate in the biosynthesis of coenzyme A (CoA) from pantothenic acid (vitamin B5). It is phosphorylated by CoA synthase in humans to form CoA. 3'-Dephosphocoenzyme A can be used as a transcription initiator in the synthesis of CoA-RNA by in vitro transcription.

Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg/kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseline within seven days post-treatment. Formulations containing abarelix have previously been used in the treatment of advanced prostate cancer.

Melanotan II acetate is an agonist of melanocortin receptor 1 (MC1R), MC3R, MC4R, and MC5R. It has been shown to improve recovery of sciatic nerve function after mechanical injury and increase cisplatin-induced decreases in sensory nerve conduction velocity. Melanotan II acetate increases oxygen consumption and protein levels of uncoupling protein 1 (UCP1) in brown adipose tissue homogenates and decreases food intake, body weight, and serum levels of leptin, glucose, insulin, and cholesterol.

(±)-α-Tocopherol acetate is the acetate form of (±)-α-tocopherol, a biologically active form of vitamin E. It prevents reductions in the percentage of embryos developing into blastocysts, levels of glutathione (GSH), and prevents increases in oxidative stress. (±)-α-Tocopherol acetate has been shown to prevent body weight loss and decreases in pulmonary dynamic compliance in mice exposed to sidestream cigarette smoke but not in sham exposure animals. However, it also increases the levels of IL-1β, IL-4, and IFN-γ in the bronchoalveolar lavage fluid (BALF) of sidestream cigarette-exposed, but not sham exposure, mice.

GHRP-6 acetate is a synthetic growth hormone (GH) secretagogue and an agonist of the GH secretagogue receptor (GHS-R), which is also known as the ghrelin receptor. It inhibits binding of the GHS-R agonist MK-0677 (Ibutamoren) to COS-7 cell membranes expressing human GHS-R type Ia and binding of ghrelin to COS-7 cells expressing human GHS-R. GHRP-6 stimulates intracellular calcium mobilization in BHK cells expressing the human receptor and inositol phosphate production in COS-7 cells expressing the human receptor. It also acts as a negative allosteric modulator of ghrelin signaling. GHRP-6 induces release of GH, but not thyroid-stimulating hormone (TSH), luteinizing hormone (LH), or follicle-stimulating hormone (FSH), in isolated rat pituitary gland. It increases levels of GH, but not TSH, LH, FSH, or prolactin, in rat blood when administered subcutaneously at a dose of 50 μg. GHRP-6 increases food intake in rats when administered intracerebroventricularly at 0.3, 1, and 3 nmol.

SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ. It binds to PPARα and PPARγ but does not bind to PPARβ/δ. It increases transcriptional activity of PPARα and PPARγ and glucose consumption. MD001 decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.

trans-ε-Viniferin is a stilbene polyphenol and dimer of trans-resveratrol that has been found in various red wines. It induces disaggregation of aggregated amyloid-β (1-42) (Aβ42) fibrils and decreases Aβ42- and IL-1β-induced release of TNF-α and IL-6 in primary mouse neuron and astrocyte cocultures. trans-ε-Viniferin reduces cytotoxicity induced by truncated huntingtin (Htt) in PC12 cells. It also reduces production of reactive oxygen species (ROS), mitochondrial dysfunction, and PGC-1α depletion and increases protein levels and deacetylase activity of sirtuin 3 (SIRT3) in cells expressing mutant Htt. trans-ε-Viniferin inhibits calcium-activated chloride channel currents in HT-29 cells. In vivo, trans-ε-viniferin reduces rotavirus-induced secretory diarrhea in mice without affecting the rotaviral infection. Dietary administration of trans-ε-viniferin reduces hepatic triglyceride accumulation and body weight increases in a mouse model of diet-induced obesity.

TP-238 HCl is a chemical probe for the bromodomains of cat eye syndrome chromosome region, candidate 2 (CECR2) and bromodomain PHD finger transcription factor (BPTF). TP-238 binds to CECR2 and BPTF with KD values of 10 and 120 nM, respectively, in an isothermal titration calorimetry (ITC) assay and IC50 values of 30 and 350 nM, respectively, in an AlphaScreen? assay.

CAY10729 TFA is a tetrazole derivative of the protein arginine deiminase (PAD) inhibitor Cl-amidine that selectively inhibits PAD1 over PAD2, PAD3, and PAD4.

GHK-Cu acetate is a complex of the tripeptide Gly-His-Lys and a copper(II) ion that has wound healing and anti-inflammatory activities. It increases proliferation and the levels of collagen and secreted pro-matrix metalloproteinase-2 (MMP-2) in isolated human fibroblasts. GHK-Cu increases levels of collagen and glycosaminoglycans (GAGs) and the expression of decorin in the wound tissue of rats. It decreases LPS-induced increases in the levels of reactive oxygen species (ROS), IL-6, and TNF-α in RAW 264.7 cells when used at a concentration of 10 μM.3 GHK-Cu (10 μg/g) prevents LPS-induced decreases in lung superoxide dismutase (SOD) activity and glutathione (GSH) levels and reduces LPS-induced increases in the number of cells and the level of total protein in bronchoalveolar lavage fluid (BALF) in a mouse model of acute lung injury.

LH1306 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1. It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1.

GKK1032B is a fungal metabolite that has antiproliferative and antibacterial activities. GKK1032B inhibits the growth of HeLa S3 cervical and MCF-7 breast cancer cells and Vero cells. It also inhibits the growth of B. subtilis and M. tuberculosis.

Gliovirin is a fungal metabolite with fungicidal, antimicrobial and anti-inflammatory activities. It is active against the plant pathogenic fungus P. ultimum and the parasite T. brucei brucei, but has no effect on the plant pathogenic fungi R. solani, P. omnivorum, T. basicola, R. arrhizus, and V. dahliae or the bacteria B. thuringiensis, P. fluorescens, and X. malvacearu. Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 and protein levels of IL-2 in Jurkat cells.

Selank acetate is a synthetic derivative of the tetrapeptide tuftsin with anxiolytic and anti-inflammatory activities.

Prostaglandin D synthase (hematopoietic-type) inhibitor F092 is an inhibitor of hematopoietic-type prostaglandin D synthase (H-PGDS).

Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus.

Bacopasaponin C is a triterpenoid saponin that inhibits the ATPase activity of P-glycoprotein.

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite with antioxidant, antiproliferative, antibacterial, and antiviral properties. 2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria. It also inhibits HIV-1 integrase in both coupled and strand transfer assays.

N6-Ethyladenosine is an adenosine A1 and A3 receptor agonist. N6-Ethyladenosine completely inhibits forskolin-induced cAMP accumulation in CHO cells expressing the human recombinant adenosine A3 receptor.

A2AR agonist-1 is an agonist of the adenosine A2A receptor and an inhibitor of equilibrative nucleoside transporter 1 (ENT1). A2AR agonist-1 also rescues motor performance and increases survival in a transgenic mouse model of Huntington’s disease.

Dihydrocaffeic acid is a polyphenol with antioxidant, neuroprotective, and enzyme inhibitory properties. Dihydrocaffeic acid scavenges ABTS and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals and increases the survival of RGC-5 mouse retinal ganglion cells under hypoxic conditions and in the presence of S-nitroso-N-acetyl-D,L-penicillamine (SNAP). It also decreases endothelial nitric oxide synthase (eNOS) activity and decreases infarct size in a rat model of transient ischemia induced by middle cerebral artery occlusion (MCAO).

Alaproclate HCl is a selective serotonin reuptake inhibitor (SSRI). It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum. Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons.

Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid (CSF) of sleep-deprived cats. It inhibits rat microsomal epoxide hydrolase. Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2). In vivo, Elaidamide induces physiological sleep in rats.

S-32212 HCl is an inverse agonist of the serotonin (5-HT) receptor subtypes 5-HT2CINI and 5-HT2CVSV. It is also an antagonist of the 5-HT2A receptor and the α2B-adrenergic receptor. S-32212 HCl decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats. It reduces immobility time in the forced swim test and decreases marble burying in mice and rats indicating anti-depressant-like and anxiolytic activities.

Oleanolic acid acrylate (OAA) is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A and a derivative of oleanolic acid. It is also a selective inhibitor of MAO-A with anti-depressant-like and anxiolytic activities.

NAP-1 is a compound with anesthetic activity. It increases paired-pulse inhibition in the CA1 region of the hippocampus.

Dihydrokainic acid is an inhibitor of excitatory amino acid transporter 2 (EAAT2). EEAT2 exhibits anti-depressant-like activity --- an effect that is blocked by the AMPA receptor antagonist NBQX and the serotonin (5-HT) receptor subtype 5-HT1A antagonist WAY-100635. It also increases glutamate and serotonin levels and the expression of c-Fos in the dorsal raphe nucleus. It also impairs memory acquisition, consolidation, and retrieval.

(-)-Bicuculline methochloride is an enantiomer of the GABA antagonist (+)-bicuculline methochloride. It increases the firing rate in rat cortical neurons similar to the (+) isomer but lacks GABA antagonist activity. (-)-Bicuculline methochloride inhibits sodium-independent GABA receptor binding with an IC50 value of 500 μM, which is approximately 100-fold less potent than (+)-bicuculline methochloride, but there is no stereoselectivity for sodium-dependent GABA receptor binding.

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimental autoimmune encephalomyelitis (EAE). It also decreases serum levels of lactate dehydrogenase as well as hepatic lipid peroxidation, oxidative DNA damage, and PARP levels.

Peonidin 3-O-glucoside is a metabolite of cyanidin 3-glucoside and an anthocyanin with antioxidant, anti-inflammatory, antiproliferative, and anti-metastatic properties. Peonidin 3-O-glucoside inhibits IL-1β-induced phosphorylation of IKKα, IκBα, and ERK in human articular chondrocytes. Peonidin 3-O-glucoside inhibits the growth of Hs578T human breast cancer cells in vitro in a concentration-dependent manner and decreases pulmonary metastasis in a mouse model of Lewis lung carcinoma.

Vulpinic acid is a lichen metabolite with diverse biological activities. It is active against C. perfringens, B. vulgatus, B. fragilis, B. loescheii, P. acnes, E. faecium, and methicillin-susceptible and -resistant S. aureus. Vulpinic acid prevents UVB-induced apoptosis, cytotoxicity, and cytoskeletal modifications in HaCaT human keratinocytes. It also increases scratch wound healing of HaCaT cells. Vulpinic acid reduces hydrogen peroxide-induced production of reactive oxygen species (ROS) and cytotoxicity in human umbilical vein endothelial cells (HUVECs).

STY-BODIPY is a styrene-conjugated fluorogenic probe for radical-trapping antioxidant (RTA) activity. Co-autoxidation of the STY-BODIPY signal carrier and a hydrocarbon co-substrate can be quantified by monitoring the loss of absorbance at 571 nm. STY-BODIPY has been used to measure the activity of RTAs, as well as the kinetics and stoichiometry of RTA reactions in cell-free assays.

AP-14145 HCl is a KCa2 (small conductance Ca2±activated potassium) channel negative allosteric modulator. AP-14145 HCl triples the EC50 of Ca2+ on KCa2.3 channelsand prolongs atrial effective refractory period (AERP). It also reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period.

LP-922056 is a Notum pectinacetylesterase inhibitor which activates wnt signalling. LP-922056 increases cortical bone thickness in a mouse model of bone growth.

TAT-GluA2 3Y is an Inhibitor of AMPA receptor endocytosis. Induces increased hind paw withdrawal latencies following thermal and mechanical stimuli in rats. Also exhibits antinociceptive effects in a rat model of neuropathic pain. Rescues pentobarbital-induced memory retrieval deficits in a rat model of learning and memory.

BTD is a selective TRPC5 activator with selectivity for TRPC5 over other TRP channels. BTD also activates TRPC1:5 and TRPC4:5 heteromers.

PDD-00017272 is a potent poly (ADP ribose) glycohydrolase (PARG) inhibitor.

4-Thiouridine, also known as 4-SU, is a photoactivatable ribonucleoside analog that is widely used for RNA analysis, including short-range RNA-RNA crosslinking and nascent RNA labeling. The crosslinking thio moiety is attached directly to the nucleotide base, thus 4-SU differs from uridine only by a single sulfur substitution. This offers the advantage of incorporating into an RNA chain with minimal structural perturbation and with similar base-pairing properties, reducing the likelihood that substitution will impair RNA interactions or activities.

Thalidomide-PEG3-ethylamine is a functionalized cereblon ligand for PROTAC research and development. Thalidomide-PEG3-ethylamine incorporates an E3 ligase ligand plus a short PEG linker ready for conjugation to a target protein ligand.

aTAG 2139 (CFT-2139) is an aTAG-based MTH1 fusion protein degrader with a DC50 value of 1.1 nM. aTAG 2139 has a Ki value of 2.1 nM for MTH1.

LDV is an α4β1 integrin (VLA-4) ligand and non-fluorescent derivative of LDV FITC.

J-2156 is a high affinity human somatostatin receptor 4 (sst4) agonist that reduces inflammatory airway hyperresponsiveness in acute and chronic airway inflammation. J-2156 also exhibits anxiolytic effects.

L-Buthionine sulfoximine is an irreversible γ-glutamylcysteine synthetase (γ-GCS) inhibitor that depletes glutathione levels by inhibiting synthesis. L-Buthionine sulfoximine also induces ferroptosis in vitro.

VH032 phenol - linker 2 is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. It incorporates an E3 ligase ligand plus an alkyl linker ready for conjugation to a target protein ligand.

cis VH 032, amine dihydrochloride is a negative control for the functionalized VHL ligand VH 032, amine.

Reparixin L-lysine salt is a potent and noncompetitive CXCR1 and CXCR2 allosteric antagonist that inhibits migration of neutrophils induced by CXCL1, CXCL2, CXCL8 and CINC-1. This product also inhibits vascular permeability and neutrophil recruitment in in vivo models of mild and severe ischemia/reperfusion injury. Also selectively depletes cancer stem cells in human breast cancer cell lines and xenograft models.

AM-12 is a TRPC5 inhibitor and Galangin derivative that inhibits effects of TRPC5 activator (-)-Englerin A but potentiates effects of physiological activators Sphingosine-1-phosphate and LPC.

Urapidil HCl is an antagonist of α1-adrenergic receptors (α1-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. Urapidil HCl inhibits cAMP accumulation induced by forskolin. It is also a β1-AR antagonist that inhibits the positive chronotropic response induced by isoproterenol. Urapidil HCl lowers mean arterial pressure (MAP) in anesthetized cats, an effect that is reduced by central administration of the 5-HT1A receptor antagonist spiroxatrine.

N,N-Dipropyldopamine HBr is a dopamine receptor agonist. It decreases dihydrophenylalanine (DOPA) levels in the limbic forebrain and striatum as well as reduces homovanillic acid (HVA) levels. N,N-Dipropyldopamine reduces spontaneous locomotor activity in mice, an effect that can be reversed by the antipsychotic spiroperidol.

HTMT is a histamine H1 receptor agonist that binds to the histamine H4 receptor but does not increase calcium mobilization. HTMT increases intracellular calcium and inositol phosphate levels as well as proliferation of cholangiocytes.

Obafluorin is a β-lactone antibiotic that has been found in P. fluorescens. It is active against S. aureus, S. faecalis, K. pneumoniae, and P. vulgaris.

NSC-207895 is an inhibitor of the p53-binding protein MDMX. NSC 207895 decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21). It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines selectively over wild-type and p53-null osteosarcoma cells

GHRP-2 TFA is an orally bioavailable synthetic growth hormone (GH) secretagogue and an agonist of the GH secretagogue receptor (GHS-R), which is also known as the ghrelin receptor. It induces GH release from pituitary cells and binds to hypothalamic membranes. GHRP-2 TFA also increases food intake and weight gain.

ICAAc is a solvatochromic fluorescent pH probe. As the polarity of the solvent increases, the emission wavelength of ICAAc increases. It displays excitation/emission maxima of 466/553, 431/515, and 418/503 nm in water, dioxane, and hexane, respectively. The absorption maximum of ICAAc decreases with increasing pH. It displays absorption/emission maxima of 470/554 and 428/553 nm at pH 3 and 11, respectively, in aqueous Britton-Robinson buffer, and the fluorescence intensity increases as pH decreases. ICAAc can be used for live cell applications.

Phomalactone is a fungal metabolite that is active against various strains of plant pathogenic fungi.

BMDB HCl is an analytical reference standard intended for research and forensic applications.

Chlamydocin is a histone deacetylase (HDAC) inhibitor with anticancer properties. Chlamydocin increases acetylation of histone H3 and histone H4 and inhibits growth of A2780, Malme-3M, MCF-7, HT-29, and HeLa cancer cells. Chlamydocin also increases lifespan by 10% in a P185 mouse allograft model.

Acetylcimigenol arabinoside is a triterpene glycoside originally isolated from Cimicifuga.

Rebaudioside D is a natural non-caloric sweetener. It is a steviol glycoside metabolized by gut microbiota to steviol, a compound whose safety is widely studied.

EATC is a degradation product of the antibiotic tetracycline. It is active against Pseudomonas, Agrobacterium, Moraxella, Bacillus, and E. coli.

CAY10737 is a turn-on fluorescent probe for the detection of carbon monoxide (CO). It is selective for CO over a variety of anions, amino acids, amines, biothiols, and reactive species. In the presence of palladium (Pd) and CO, CAY10737 undergoes the Pd0-mediated Tsuji-Trost reaction to release a fluorescent compound that has absorption and emission maxima of 678/714 nm, respectively. This fluorescence can be used to detect CO production in vitro and in vivo.

TFLLR-NH2 TFA is a synthetic peptide agonist of proteinase-activated receptor 1 (PAR1) that induces calcium mobilization in dorsal root ganglion neurons. In vivo, TFLLR-NH2 stimulates plasma extravasation in the bladder, esophagus, stomach, intestine, and pancreas in wild-type, but not PAR1-/-, mice. It also reduces carrageenan-induced hyperalgesia in rats.

γ-Valerolactone is a prodrug form of γ-hydroxyvaleric acid.

Triflupromazine is a phenothiazine that binds to muscarinic receptors and inhibits serotonin (5-HT) uptake by synaptosomes. Formulations containing triflupromazine were previously used as antipsychotics.

Norlidocaine is an active metabolite of lidocaine formed via N-deethylation of lidocaine by the hepatic cytochrome P450 (CYP) isoform CYP3A4. Topical administration reduces thrombus formation in microvascular injury. Plasma levels of Norlidocaine following lidocaine administration have been used to monitor declining liver function in patients with cirrhosis.

Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity. Without photoactivation, it is a weak inhibitor of PAD2 and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro. It does not inhibit histone H3 citrullination in HEK293T cells overexpressing PAD2. However, it can rapidly be photoactivated with UV-A radiation to the more active cis-isomer, which is an irreversible, competitive inhibitor of histone H3 citrullination.

GHV sodium salt is a sedative and active metabolite of γ-valerolactone.

L-Moses HCl is an inhibitor of the p300/CBP-associated factor (PCAF) bromodomain. It displaces the PCAF bromodomain from histone H3.3 in a nanoBRET target engagement assay when used at a concentration of 5 μM.

Erythromycylamine is a macrolide antibiotic and an active metabolite of dirithromycin. It is active against a variety of bacteria, including strains of S. pyogenes, S. pneumoniae, L. monocytogenes, and B. pertussis. It is also active against 28 clinical isolates of M. avium complex (MAC) isolated from patients with AIDS. Erythromycylamine inhibits polylysine and polyproline synthesis in a cell-free assay.

Micronomicin sulfate is an aminoglycoside antibiotic originally isolated from Micromonospora. It is active against S. aureus, B. subtilis, B. cereus, E. coli, and K. pneumoniae.

Biotinyl tyramide is a reagent used for tyramide signal amplification (TSA) via catalyzed reporter deposition (CARD). In CARD, a reporter enzyme, such as horseradish peroxidase (HRP) conjugated to a secondary antibody, is bound to the target of interest and catalyzes the covalent deposition of biotinyl tyramide to the sample. The sample is then probed by a detector, such as streptavidin-HRP, allowing detection via chromogenic or fluorescent methods. Biotinyl tyramide has been used in immunohistochemistry, ELISA, Western blot, and in situ hybridization applications.

Dansyl chloride is a reactive probe for the derivatization of primary amines, including those on amino acids, peptides, and polyamines, for detection by HPLC. It has also been used for the derivatization of compounds containing phenol groups, such as steroids, for detection by MS/MS. Dansyl chloride is a fluorescent probe for proteins and enzymes. It displays excitation/emission maxima of 340/535 nm, respectively, in acetone.

Siamycin I is a tricyclic peptide with antiviral and antibacterial activities. It is active against HIV-1 and CBL-20 strain of HIV-2. Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells. It is also active against B. subtilis, M. luteus, and S. aureus. Siamycin I inhibits autophosphorylation of the E. faecalis quorum sensing kinase FsrC induced by gelatinase biosynthesis-activating pheromone (GBAP).

cis-Entacapone is a metabolite of the catechol-O-methyltransferase (COMT) inhibitor entacapone. It is also a potential impurity found in commercial preparations of entacapone and a degradant of entacapone formed by UV light exposure.

Boromycin is a boron-containing macrolide antibiotic that inhibits growth of B. subtilis and induces efflux of potassium ions from B. subtilis without affecting Na+/K±ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis, inhibits the growth of B. halodurans, and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromycin reverses bleomycin-induced cell cycle arrest at the G2 phase in Jurkat cells. It inhibits replication of the HIV-1 strains LAV-1 and RF and the HIV-2 strain LAV-2 in MT-4 cells. It also inhibits replication of a clinical isolate of HIV-1, strain KK-1, in MT-4 cells and peripheral blood mononuclear cells.

Lariatin A is an antimycobacterial lasso peptide active against M. tuberculosis and M. smegmatis. Lariatin A increases survival in a silkworm model of M. smegmatis infection.

Desacetyl cefapirin is an active metabolite of the cephalosporin antibiotic cefapirin. Desacetyl cefapirin is active against E. coli, K. pneumoniae, P. mirabilis, and S. aureus.

Phenelfamycin E is an antibiotic active against β-hemolytic Streptoccus, S. pneumoniae, C. difficile, C. perfringens, and P. magnus Gram-positive bacteria. Phenelfamycin E increases survival in a mouse model of lethal S. pyogenes infection in a dose-dependent manner. Dietary administration of phenelfamycin E increases body weight in chickens.

GHK is a peptide released during extracellular matrix (ECM) protein degradation following tissue injury. It binds to copper to form GHK-Cu, a complex with diverse biological activities, including roles in tissue remodeling and wound healing, hair growth, and suppression of inflammation. GHK increases keratinocyte proliferation in vitro, as well as the number of cells positive for the keratinocyte stem cell marker p63 and the protein levels of integrin α6 and β1 in a skin equivalent model. It also reduces infiltration of inflammatory cells and decreases TNF-α and IL-6 protein levels in bronchoalveolar lavage fluid (BALF) in a mouse model of pulmonary fibrosis induced by bleomycin.

Oleoyl-D-lysine sodium is an inhibitor of glycine transporter 2a (GlyT2a). It selectively inhibits GlyT2a over GlyT1b and reduces allodynia in a nerve ligation rat model of neuropathic pain.

Pal-GHK is a form of the extracellular matrix-derived peptide GHK containing palmitic acid, which allows it to penetrate the stratum corneum to the epidermal and dermal skin layers. Pal-GHK increases collagen synthesis in skin fibroblasts. It has been used with the zwitterionic surfactant C12 dodecyldimethylamine oxide (C12DMAO) to study self-assembly of the mixture into aggregates, ribbons, and nanobelts. Pal-GHK has also been used as an internal standard for the quantification of pal-KTTKS in anti-wrinkle creams by LC-MS/MS.

Desertomycin A is fungal metabolite and the major component of the desertomycin antibiotic complex.

Squalene is a biosynthetic precursor to all steroids. An oil-in-water emulsion of squalene synergistically increases adaptive immune responses to glucopyranosyl lipid adjuvant (GLA), a toll-like receptor 4 (TLR4) agonist, compared with an aqueous formulation of GLA. Formulations containing squalene have been used as adjuvants in vaccines and as hair and skin conditioning agents.

Alfrutamide is a phenolic amide that has diverse biological activities including anti-inflammatory, antioxidative, and antiproliferative properties. It decreases nitric oxide (NO) production and inducible NO synthase (iNOS) activity and increases NO scavenging without inducing cytotoxicity. It also scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals in TLC autographic and spectrophotometric assays.

Feglymycin is a 13-amino acid peptide that has antibacterial and antiviral activities. It is active against Gram-positive bacteria and inhibits HIV viral replication.

Imidocarb propionate is an antiprotozoal agent that eliminates blood parasites. Formulations containing imidocarb have been used in the veterinary treatment of babesiosis and other protozoal infections.

PBD-BODIPY is a probe for the spectrophotometric measurement of autoxidation reactions. Co-autoxidation of the PBD-BODIPY signal carrier and a hydrocarbon co-substrate can be quantified by monitoring loss of absorbance at 591 nm.

Roridin L2 is a fungal metabolite.

Neoeriocitrin is a flavonoid that has antioxidative and osteogenic activities. It inhibits the production of DPPH radicals and the formation of superoxide radicals. Neoeriocitrin increases proliferation of MC3T3-E1 osteoblast percursor cells and reverses the antiproliferative effect of the MEK1 inhibitor PD 98059. It also increases the expression of the osteogenic differentiation markers Runx2, Type 1 collagen, and osteocalcin.

Terlipressin is a prodrug form of lysipressin and a partial agonist of the vasopressin V1A receptor. It is also an agonist of vasopressin V1B and V2 receptors. Terlipressin in combination with norepinephrine improves vascular reactivity and mean arterial pressure (MAP) in a rat model of liver cirrhosis with portal hypertension, arterial hypotension, high cardiac output, and low systemic vascular resistance.

β-Apooxytetracycline is a potential impurity of oxytetracycline. β-Apooxytetracycline is a degradation product formed from oxytetracycline via acid hydrolysis. β-Apooxytetracycline is toxic to rats, decreasing body weight, disrupting blood cell counts, and inducing hepatocyte necrosis.

Axitinib N-Glucuronide is a metabolite of the receptor tyrosine kinase inhibitor Axitinib. It is formed via glucuronidation of axitinib by the UDP-glucuronosyltransferase (UGT) isoform UGT1A1.

Trilobatin is a dihydrochalcone glucoside and derivative of phloretin that reduces survival of Bel 7402 and HepG2 cancer cells. Trilobatin increases superoxide dismutase (SOD) and glutathione peroxidase (GPX) activity and inhibits lipid peroxidation. Pretreatment with trilobatin reduces hydrogen peroxide-induced cell death and production of mitochondrial reactive oxygen species (ROS), prevents reduction in the mitochondrial membrane potential, and increases the activity of GPX, SOD2, and isocitrate dehydrogenase 2 (IDH2) in PC12 neuronal cells. Trilobatin inhibits infection by various HIV-1 strains without inducing cytotoxicity in target cells.

Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Upon enzymatic cleavage by the 26S proteasome or 20S proteolytic core, amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify 26S proteasome or 20S proteolytic core trypsin-like activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.

CAP 3 is a cholic acid-peptide conjugate (CAP) with antibacterial activity. It is active against the Gram-negative bacteria E. coli, K. pneumoniae, and A. baumanii. CAP 3 increases the fluidity of model Gram-negative bacterial membranes and binds to LPS in vitro. It reduces the biomass and number of colony-forming units in E. coli biofilms in a concentration-dependent manner. It is cytotoxic to A459 cells and has hemolytic activity against human red blood cells.

Neoxaline is an alkaloid fungal metabolite.

Rugulotrosin A is an antibiotic active against the Gram-positive bacteria E. faecalis, B. cereus, B. subtilis, and S. aureus. Rugulotrosin A is inactive against Gram-negative bacteria.

Cholesteryl palmitate is a cholesterol ester used to form a stable tear film to study amphiphilic block copolymers as surfactants for dry eyes. Cholesteryl palmitate levels in amniotic fluid are decreased in pregnancies in which infants later developed respiratory distress syndrome and in patients with well-controlled diabetes. Levels of cholesteryl palmitate are increased in bronchoalveolar lavage fluid (BALF) from patients with chronic interstitial pneumonia.

Pyridoxatin is a fungal metabolite that inhibits production of thiobarbituric acid reactive substance (TBARS). Pyridoxatin inhibits hemolysis induced by the free radical generator AAPH and is active against C. albicans.

Antibiotic PF 1052 is a fungal metabolite active against S. aureus, S. parvulus, and C. perfringens. It inhibits neutrophil migration, reduces pseudopodia formation, and induces rounding of neutrophils. Antibiotic PF 1052 is selective for neutrophil migration over macrophage migration in zebrafish larvae. It also inhibits the migration of murine neutrophils.

Zelkovamycin is a cyclic peptide antibiotic that inhibits growth of X. oryzae, P. oryzae, S. aureus, and A. laidlawii in a concentration-dependent manner.

Epioxytetracycline is a degradation product of the antibiotic oxytetracycline.

Silodosin glucuronide sodium is an active metabolite of the α1A-adrenergic receptor antagonist silodosin. It is formed from silodosin by the UDP-glucuronosyltransferase (UGT) isoform UGT2B7.

Peimisine HCl is a steroidal alkaloid that inhibits lung acetylcholinesterase (AChE).

ABTS is a radical cation and a peroxidase substrate. It is used to assess antioxidant capacity in the Trolox equivalent antioxidant capacity (TEAC) assay. It is blue in the presence of sodium persulfate or metmyoglobin but decolorizes upon incubation with antioxidants, and the antioxidant capacity can be determined spectrophotometrically. ABTS has also been used as an enzyme substrate in ELISAs. Upon incubation with a peroxidase, it produces a soluble green product that can be quantified by colorimetric detection at 405 nm.

Verrucofortine is a fungal metabolite.

Reduced haloperidol is an active metabolite of haloperidol formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake.

Steffimycin B is an anthracycline bacterial metabolite. It binds to DNA, preferentially intercalating at sites containing cytosine and guanine. Steffimycin B is cytotoxic to MCF-7, KB, NCI-H187, and Vero cells. It is active against M. tuberculosis, B. cereus, and P. falciparum.

Integracin B is a fungal metabolite and an inhibitor of HIV-1 integrase.

Tenellin is a fungal metabolite that inhibits Mg2±, Ca2±, and Na+/K±ATPase activities in erythrocytes. Tenellin is cytotoxic to Sf9 and Sf21 insect cells.

Hygrolidin is a macrocyclic lactone that inhibits proliferation of DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells. Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovani, and T. b. brucei but also induces cytotoxicity in HepG2 cells.

N-methyl Mesoporphyrin IX is a transition state analog of porphyrin and an inhibitor of ferrochelatase. N-methyl Mesoporphyrin IX has been used as a turn-on biosensor for target DNA sequences when used in complex with a G-quadruplex-forming sequence fused to a DNA sequence complementary to the target sequence. It has also been used to detect amyloid-β (1-40) (Aβ40) fibrils in vitro and in live PC12 cells overexpressing Aβ.

Pipacycline is a tetracycline antibiotic derivative. It inhibits the formation of penicillinase, the enzyme that inactivates penicillin in bacteria. It decreases oxygen uptake and inhibits growth of penicillin-resistant penicillinase-producing S. aureus.

Deethylindanomycin is a polyether antibiotic that is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae. It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when. Deethylindanomycin acts as an ionophore in lipid bilayer membranes and is more selective for potassium ions than calcium, magnesium, and sodium ions. It induces histamine release from rodent mast cells and human basophils in vitro in a calcium-dependent manner.

TAN 420E is a bacterial metabolite that scavenges DPPH radicals and reduces thiobarbituric acid reactive substances (TBARS) liver microsomes. TAN 420E is active against B. brevis, B. cereus, M. flavus, and S. aureus. It is cytotoxic to P388 and KB lymphocytic leukemia cells.

Sporidesmolide II is a cyclic depsipeptide.

Spinosyn A aglycone is an aglycone form of the insecticide spinosyn A. It is formed by acid hydrolysis of spinosyn A 17-pseudoaglycone and has no insecticidal activity at concentrations up to 64 ppm.

Neoaureothin is a bacterial metabolite and androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells. It also has nematocidal activity against the pine wood nematode B. xylophilus and increases survival of P. densiflora trees inoculated with B. xylophilus.

SCH 38519 is an isochromanequinone fungal metabolite that inhibits aggregation induced by thrombin as well as serotonin secretion in human platelets. It inhibits the growth of various Gram-negative and Gram-positive bacteria.

Nybomycin is a fungal metabolite with antibacterial activity. It is active against B. subtilis, B. cereus, B. mycoides, M. smegmatis, and K. pneumoniae. Nybomycin is also active against M. tuberculosis and M. bovis.

Avenaciolide is a water-insoluble fungal metabolite that inhibits glutamate transport in isolated rat liver mitochondria.

LysoFP-NH2 is the fluorescent form of the lysosomal turn-on fluorescent probe for carbon monoxide (CO) lysoFP-NO2. LysoFP-NH2 is formed when lysoFP-NO2 reacts with CO. It displays excitation/emission maxima of 440/528 nm, respectively.

MGR2 is a negative control compound for the activity of the reactive oxygen species-generating probe MGR1. Unlike MGR1, MGR2 does not induce superoxide production or cell death in HEK293T cells.

Deoxyfusapyrone is an α-pyrone fungal metabolite that has antifungal activity. It is active against C. neoformans, A. fumigatus, A. niger, and A. flavus human mycoses. Deoxyfusapyrone is also active against a variety of filamentous fungi, but not yeast or the bacterium B. megaterium.

TAN 1364B is a protein tyrosine phosphatase (PTP) inhibitor and the racemic and monomeric form of RK-682. TAN 1364B inhibits the activity of the PTPs LMW-PTP, CDC25B, and PTP1B, but the inhibitory activity against LMW-PTP and CDC25B is blocked in the presence of magnesium. TAN 1364B forms aggregates in solution and binds to both the PTP binding site and to protein surfaces.

Collismycin A is a bacterial metabolite with antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria and fungi. It inhibits proliferation of A549 lung, HCT116 colon, HeLa cervical cancer cells, and NIH373 fibroblasts but not MDA-MD-231 breast cancer cells. Collismycin A forms a complex with Fe(II) and Fe(III) at a 2:1 ratio, and the addition of iron ions inhibits the antiproliferative effect of collismycin A on HeLa cells, an effect that does not occur with the addition of zinc, manganese, copper, or magnesium ions. Collismycin A (1 μM) prevents apoptosis in the brain region of zebrafish larvae by 44% in a model of neuronal cell death induced by all-trans retinoic acid.

Demethoxyviridiol is a mycotoxin that inhibits phosphatidylinositol 3-kinase (PI3K).

Brevicompanine B is a fungal metabolite that has plant growth and circadian rhythm regulatory activity. Brevicompanine B inhibits primary root growth in Arabidopsis seedlings and disrupts the transcription of various genes involved in the regulation of plant circadian rhythm. It is active against P. falciparum.

MAGL Inhibitor Compound 23 is an inhibitor of monoacylglycerol lipase (MAGL). It is selective for MAGL over cannabinoid receptor 1 (CB1), CB2, fatty acid amide hydrolase (FAAH), α/β-hydrolase domain-containing protein 6 (ABHD6), and ABHD12. MAGL inhibitor compound 23 inhibits the growth of HCT116, MDA-MB-231, Caov-3, OVCAR-3, and SKOV3 cells but not MRC5 cells. It increases the levels of 2-arachidonoyl glycerol (2-AG) in mouse brain and plasma when administered at a dose of 50 mg/kg.

Antibiotic TS 885 is a microbial metabolite that has antifungal and antiviral activities. It is active against several fungi, including S. sake, S. fragilis, R. rubra, T. rubra, and C. albidus and has antiviral activity against poliovirus, vesicular stomatitis virus (VSV), and Newcastle disease virus (NDV) in vitro. 9-Methylstreptimidone increases survival in mouse models of infection with influenza A2 (H2N2) or C. albicans when administered prior to infection.

K-TMZ is a DNA alkylating agent. It increases the concentration of O6-methylated deoxyguanosine in U87 glioblastoma multiforme (GBM) cells in a concentration-dependent manner. K-TMZ reduces cell viability of GBM cell lines lacking or expressing O6-methylguanine DNA methyltransferase (MGMT).

Meclocycline is a tetracycline antibiotic with broad antimicrobial activity. Meclocycline inhibits lactate dehydrogenase (LDH) release and cell toxicity induced by expression of htt-N63-148Q, a mutant form of the huntingtin gene, without altering htt-N63-148Q protein levels in PC12 cells.

(+)-Quinolactacin A1 is a fungal metabolite that inhibits acetylcholinesterase (AChE).

SPQ is a fluorescent chloride indicator. It has been used to assess voltage-sensitive chloride transport in placental microvillus vesicles. It has also been used to continuously quantify intracellular calcium efflux induced by parathyroid hormone, forskolin, and PMA in isolated human erythrocytes. In addition, SPQ has been used to determine the type of ion conductance induced by the cystic fibrosis transmembrane conductance regulator (CFTR) in HEK293 cells expressing pTrial10-CRTR2.

Acetaminophen glucuronide is an inactive metabolite of the analgesic and antipyretic agent acetaminophen. It is formed via glucuronidation of acetaminophen by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A6, UGT1A9, UGT1A1, and UGT2B15.

Iloperidone metabolite P88 is an active metabolite of the atypical antipsychotic iloperidone. It binds to the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT2A, and 5-HT2C, α2b- and α2c-adrenergic, and dopamine D1, D2A, and D4 receptors.

FINO2 is a ferroptosis-inducing peroxide compound that indirectly inhibits glutathione peroxidase 4 (GPX4) and oxidizes iron. It decreases GPX4 activity and protein levels in vitro but does not act as an active site, allosteric, or covalent inhibitor of GPX4 or alter GPX homeostasis. It also oxidizes iron in vitro, leading to degradation of the endoperoxide moiety, but does not affect the protein levels of iron regulatory proteins, such as IRP2, FTL1, or TFR. FINO2 induces lipid peroxidation of a large subset of the lipidome in HT-1080 cells when used at a concentration of 10 μM and induces ferroptosis in an arachidonic acid lipoxygenase-independent manner. It inhibits cell growth and induces lethality in the NCI-60 panel of cancer cell lines. It is selective for oncogenically transformed BJ-ELR cells over noncancerous BJ-hTERT cells. FINO2 induces oxidative stress, including lipid peroxidation, in RS4;11 B-lymphoblastic leukemia cells. It induces iron-dependent cell death, an effect that can be blocked by pretreatment with the lipophilic antioxidants ferrostatin-1 and liproxstatin-1 and does not induce markers of apoptosis, necrosis, or autophagy in RS4;11 cells.

Sorafenib N-oxide is an active metabolite of sorafenib (BAY 43-9006), an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD. It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3. Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4.

BB-F-Yne is a cell-permeable derivative of the protein arginine diminase (PAD) inhibitor BB-Cl-amidine that contains an alkyne moiety for use in click chemistry reactions. BB-F-Yne inhibits PAD1-4 and has been used for labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.

UF-17 HCl is an analytical reference standard that is structurally similar to known utopioids.

α-hydroxy Metoprolol is an active metabolite of the β1-adrenergic receptor blocker metoprolol. It is formed via metabolism of metoprolol by the cytochrome P450 (CYP) isoform CYP2D6.

Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs). Streptochlorin prevents degranulation in antigen-stimulated mast cells, as well as inhibits Syk kinase and the Src family kinases LYN and Fyn and reduces the secretion of TNF-α and IL-4 induced by dinitrophenyl-human serum album (DNP-HSA) in RBL-2H3 mast cells. It also decreases swelling and reduces scratching behavior in a mouse model of allergic dermatitis induced by dinitrofluorobenzene (DNFB).

(-)-Cyclopenol is a benzodiazepine alkaloid fungal metabolite that inhibits protein tyrosine phosphatase 1B (PTP1B).

BMP-22 is an inhibitor of autotaxin. It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7. BMP-22 inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine (LPC) and inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.

Aspergillin PZ is a fungal metabolite active against S. epidermidis but not S. aureus, E. coli, or B. cereus. It is cytotoxic to HL-60 promyelocytic leukemia cells but not THP-1 acute monocytic leukemia or PC3 prostate cancer cells.

DiIC1(5) is a signal-off fluorescent probe for the detection of mitochondrial membrane potential disruption. It accumulates in mitochondria and its fluorescence intensity decreases when the mitochondrial membrane potential is disrupted. DilC1(5) has been used in combination with a variety of cell damage and cell death markers to classify nine stages of cell death using flow cytometry. It has also been used as a quencher for the detection of serine phosphorylation and tyrosine dephosphorylation post-translational modifications (PTMs) in quenching resonance energy transfer (QRET) and mTR-FRET applications. It displays excitation/emission maxima of 659/666 nm, respectively.

Calpinactam is a fungal metabolite with antimycobacterial activity. It is active against M. smegmatis.

Martinomycin is a polyether antibiotic active against a variety of bacteria including 11 strains of S. aureus, three strains of S. pneumoniae, and E. faecalis.

Aspergillimide is a fungal metabolite that reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.

Abacavir carboxylate is an inactive metabolite of the HIV-1 reverse transcriptase inhibitor abacavir. It is formed from abacavir via reactive aldehyde intermediates that can form adducts with proteins on valine residues.

Iloperidone metabolite P95 is a metabolite of the atypical antipsychotic iloperidone. It binds to the serotonin (5-HT) receptor subtype 5-HT2A and α1-, α2B-, and α2C-adrenergic receptors but does not cross the blood-brain barrier.

Avanafil metabolite M4 is a major active metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil. Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M4 and avanafil metabolite M16 as well as minor metabolites. Avanafil metabolite M4 inhibits PDE5 with 18% of the potency of avanafil.

SRS16-86 is an inhibitor of ferroptosis. It inhibits ferroptosis induced by erastin in HT-1080 and NIH3T3 cells. SRS16-86 prevents renal tubular damage and increases in serum levels of urea and creatine in a mouse model of renal ischemia-reperfusion injury (IRI). In a rat model of spinal cord injury, SRS16-86 increases the levels of glutathione peroxidase 4 (GPX4), system xc- cystine/glutamate transporter (xCT), and glutathione (GSH) and decreases levels of IL-1β, TNF-α, ICAM-1, and the lipid peroxidation marker 4-hydroxy nonenal (4HNE) in injured spinal cord epicenters. It also increases tissue sparing and improves locomotor recovery in the same model.

3-hydroxy Darifenacin is a metabolite of darifenacin. It is an antagonist of M1-5 muscarinic receptors.

Avanafil metabolite M16 is a major inactive metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil. Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M16 and avanafil metabolite M4 as well as minor metabolites.

BODIPY 558/568 C12 is a fatty acid-conjugated fluorescent probe for lipid droplets. It displays excitation/emission maxima of 558/568 nm, respectively, and has been used to monitor the localization and dynamics of lipid droplets in live cells.

YnMyr Diazirine X10 is a cell-permeable photoreactive probe for protein myristoylation.1,2 It contains a terminal clickable alkyne moiety and a photoactivatable diazirine group at carbon 10 that allow its incorporation into myristylated proteins and photo-activated cross-linking of their interacting partners, respectively.

BB-Cl-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine that contains an alkyne moiety for use in click chemistry reactions. BB-Cl-Yne inhibits PAD1-4 and has been used for labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.

NG-25 HCl hydrate is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner. It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer.

(±)-Ketoprofen glucuronide is a phase II metabolite of the non-steroidal anti-inflammatory drug (NSAID) ketoprofen. It is formed via glucuronidation by the UDP-glucuronosyltrasferase (UGT) isoforms UGT1A3, UGT1A9, UGT1A10, and UGT2B7.

Chrodrimanin B is a meroterpenoid fungal metabolite with insecticidal activity against third instar silkworm larvae.

Pyranonigrin A is a fungal metabolite with antioxidant activity. It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals in a cell-free assay. Pyranonigrin A suppresses TNF-α-induced expression of vascular cell adhesion molecule 1 (VCAM-1) in human umbilical vein endothelial cells (HUVECs).

(-)-Rasfonin is a fungal metabolite that inhibits proliferation of mouse splenocytes induced by concanavalin A and LPS.

Quinolactactin A is a quinolone fungal metabolite that inhibits TNF production induced by LPS in murine peritoneal macrophages. Quinolactacin A is a mixture of quinolactacin A1 and A2.

(+)-Macrosphelide A is a fungal metabolite that inhibits adhesion of HL-60 human leukemia cells to human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner. It also inhibits the growth of SKOV3 ovarian cancer cells in a concentration-dependent manner. (+)-Macrosphelide A inhibits the growth of Gram-positive bacteria, including B. subtilis, M. luteus, B. thuringiensis, and S. aureus but not Gram-negative bacteria or fungi.

NG 012 is a fungal metabolite with fungicidal and nerve growth factor-potentiating properties. NG 012 increases the efficacy of the antifungal miconazole against C. albicans. It also potentiates neurite outgrowth induced by nerve growth factor (NGF) in PC12 cells in a concentration-dependent manner.

OM173-αA is a quinone bacterial metabolite that inhibits the growth of the bacteria M. gallisepticum, M. pneumoniae, and S. aureus. OM173-αA also inhibits the growth of the plant pathogenic fungus P. oryzae and several species of Trichophyton.

Tenofovir diphosphate sodium salt is an inhibitor of HIV reverse transcriptase and hepatitis B virus (HBV) polymerase. It is selective for these enzymes over DNA polymerase α and β, as well as mitochondrial DNA polymerase γ. Tenofovir diphosphate is formed intracellularly through phosphorylation of the prodrugs tenofovir and tenofovir disoproxil by nucleotide kinases. Increased levels of tenofovir diphosphate in isolated peripheral blood mononuclear cells (PBMCs) correlate with a decrease in the risk of simian HIV (SHIV) acquisition in a macaque model of rectal SHIV transmission.

C11 BODIPY 581/591 is a lipid-soluble ratiometric fluorescent indicator of lipid oxidation. Upon oxidation, its excitation maximum shifts from 581 to 500 nm and the emission maximum shifts from 591 to 510 nm. C11 BODIPY 581/591 has been used in the quantitation of ferroptosis.

Ambuic acid is a cyclohexanone that has phytopathogenic antifungal, quorum sensing inhibitory, and antibacterial activities. Ambuic acid inhibits the biosynthesis of cyclic peptides involved in quorum sensing, including gelatinase biosynthesis-activating pheromone (GBAP) in E. faecalis, autoinducing peptide I (AIP-I) in S. aureus, and LsrD698 and LsrD826 in L. innocua. It suppresses abcess formation in a mouse model of skin infection induced by methicillin-resistant S. aureus (MRSA) when administered at a dose of 5 μg and decreases the activity of the agr quorum sensing system in an in vivo reporter assay.

Bostrycin is an anthraquinone with antibacterial, antiproliferative, and phytotoxic properties. It is active against Gram-positive bacteria, including methicillin-resistant S. aureus (MRSA), M. tuberculosis, and C. botulinum. Bostrycin inhibits proliferation of A549 lung adenocarcinoma cells as well as halts the cell cycle at the G0/G1 phase and induces apoptosis in A549 cells. Bostrycin has been used as a cross-linking agent for protein immobilization that retains bacteriostatic activity when immobilized on nonwoven polypropylene fabric.

SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2. It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells and decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719. SGK1 inhibitor reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.

(S)-Laudanosine is the (S) enantiomer of laudanosine, a metabolite of the neuromuscular blocking agents atracurium and cisatracurium. It inhibits prolyl endopeptidase and inhibits both arachidonic acid- and collagen-induced aggregation in washed rabbit platelets.

HAPC-Chol is a cationic cholesterol. HAPC-Chol, as part of a lipoplex with DOPE, has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in HAPC-chol accumulation in the lungs.

DC-Chol is a cationic cholesterol derivative. DC-Chol, as a component of lipoplexes with DOPE, has been used for transfection of mRNA into A549 cells without affecting cell viability. Incubation of DC-chol/DOPE liposomes or lipoplexes with human whole blood has no effect on neutrophil elastase or β-thromboglobulin levels or the number of platelets and red and white blood cells, indicating hemocompatibility. DC-Chol has also been widely used in the synthesis of liposomes for the delivery of siRNA, DNA, and chemotherapeutic agents into cells and mice.

(±)-Tocol is a synthetic vitamin E derivative. Unlike (±)-α-tocopherol, (±)-tocol does not suppress retinol-induced erythrocyte hemolysis or increase microviscosity of rat liver phosphatidylcholine (PC) liposomes.

Dihydrotetrabenazine (racemic) is an active metabolite of the vesicular monoamine transporter 2 (VMAT2) inhibitor tetrabenazine that is generated by hepatic carbonyl reductases. Dihydrotetrabenazine binds to mouse pons medulla, hypothalamus, and striatum and inhibits synaptic vesicular serotonin (5-HT) uptake. It also binds to human caudate nucleus, hippocampus, and substantia nigra pars compacta. Dihydrotetrabenazine stereoisomers bind to VMAT2 in rat striatum.

(±)-γ-Tocopherol is a form of vitamin E with antioxidant and anti-inflammatory properties. It traps and detoxifies reactive nitrogen oxide species, including nitrogen dioxide, in cell-free assays. It also reduces the synthesis of prostaglandin E2 (PGE2) induced by LPS in RAW 264.7 macrophages and by IL-1β in A549 cells. (±)-γ-Tocopherol inhibits LPS-induced nitrite release and inducible nitric oxide synthase (iNOS) expression in RAW 264.7 cells and reduces COX-2 activity in A549 cells pretreated with IL-1β. Serum levels of (±)-γ-tocopherol are decreased in patients with cardiovascular disease.

N-methyl Paroxetine is a derivative of the selective serotonin reuptake inhibitor (SSRI) antidepressant paroxetine that inhibits [3H]paroxetine binding to rat cortical membranes. It inhibits serotonin (5-HT) uptake in rat brain synaptosomes and has been used as a precursor in the synthesis of paroxetine.

Chromomycin A2 is an aureolic acid that has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs). Chromomycin A2 halts the cell cycle in the G0/G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells. This indicates that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

Territrem B is a mycotoxin that irreversibly inhibits acetylcholinesterase (AChE). It is toxic to mice, inducing tremors with a median tremulous dose of 0.21 mg/kg.

Terpendole C is an indole diterpene alkaloid fungal metabolite and inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT). It also inhibits ACAT in J774 macrophages without affecting cell growth.

p-APMSF is an irreversible inhibitor of serine proteases.

MHAPC-Chol is a cationic cholesterol. MHAPC-Chol, as part of a lipoplex with DOPE, has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in MHAPC-chol accumulation in the liver.

Tetrahydropiperine is a piperine derivative that has diverse biological activities. It is an agonist of transient receptor potential vanilloid type 1 (TRPV1). It inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH) and 7-methoxycoumarin O-demethylase (MOCD) activity in rat liver microsomes.

Ibuprofen carboxylic acid is a major metabolite of ibuprofen.

Norucholic acid is a Ursodeoxycholic Acid (U850000) derivative. It is superior to Ursodeoxycholic acid in the treatment of sclerosing cholangitis in Mdr2 (Abcb4) knockout mice.

DMPAC-Chol is a cationic cholesterol derivative that has been used in liposome formation for gene transfection. Liposomes containing DMPAC-chol bind to DNA in a band shift assay and protect against serum nuclease degradation of DNA.

Febuxostat acyl glucuronide is a metabolite of the xanthine oxidoreductase inhibitor febuxostat. Febuxostat acyl glucuronide is formed via glucuronidation of febuxostat by uridine diphosphate-glucuronosyltransferases (UGTs).

True Blue is a fluorescent neuronal retrograde tracer that labels the nucleus, nucleolus, cell body, proximal dendrites, and axons of neurons. It displays excitation/emission maxima of 373/404 nm, respectively.