| DC36271 |
MD001 |
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. |
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| DC36272 |
(-)-ε-Viniferin |
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. |
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| DC36273 |
TP-238 HCl |
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. |
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| DC36274 |
CAY10729 TFA |
CAY10729 TFA is a tetrazole derivative of the protein arginine deiminase (PAD) inhibitor Cl-amidine that selectively inhibits PAD1 over PAD2, PAD3, and PAD4. |
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| DC36275 |
GHK-Cu acetate |
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. |
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| DC36276 |
LH1306 |
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. |
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| DC36277 |
GKK1032B |
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. |
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| DC36278 |
Gliovirin |
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. |
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| DC36279 |
Selank acetate |
Selank acetate is a synthetic derivative of the tetrapeptide tuftsin with anxiolytic and anti-inflammatory activities. |
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| DC36280 |
Prostaglandin D synthase (hematopoietic-type) inhibitor F092 |
Prostaglandin D synthase (hematopoietic-type) inhibitor F092 is an inhibitor of hematopoietic-type prostaglandin D synthase (H-PGDS). |
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| DC36281 |
Pristinamycin IA
Featured
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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. |
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| DC36282 |
(-)-Bacopasaponin C |
Bacopasaponin C is a triterpenoid saponin that inhibits the ATPase activity of P-glycoprotein. |
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| DC36283 |
3-Hydroxyterphenyllin |
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. |
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| DC36284 |
N6-Ethyladenosine |
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. |
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| DC36285 |
A2AR agonist-1 |
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. |
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| DC36286 |
Dihydrocaffeic acid |
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). |
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| DC36287 |
Alaproclate HCl |
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. |
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| DC36288 |
Elaidamide |
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. |
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| DC36289 |
S-32212 HCl |
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. |
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| DC36290 |
Oleanolic acid acrylate |
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. |
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| DC36291 |
NAP-1 |
NAP-1 is a compound with anesthetic activity. It increases paired-pulse inhibition in the CA1 region of the hippocampus. |
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| DC36292 |
Dihydrokainic acid |
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. |
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| DC36293 |
(-)-Bicuculline methochloride |
(-)-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. |
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| DC36294 |
6(5H)-Phenanthridinone |
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. |
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| DC36295 |
Peonidin 3-O-glucoside |
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. |
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| DC36296 |
NSC 5897 |
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). |
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| DC36297 |
STY-BODIPY |
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. |
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| DC36298 |
AP14145 HCl |
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. |
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| DC36299 |
LP-922056 |
LP-922056 is a Notum pectinacetylesterase inhibitor which activates wnt signalling. LP-922056 increases cortical bone thickness in a mouse model of bone growth. |
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| DC36300 |
TAT-GluA2 3Y |
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. |
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