Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct.

Tigecycline hydrate is a broad spectrum glycylcycline antibiotic. Tigecycline hydrate is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline hydrate is active against resistant strains of Gram-positive and Gram-negative bacteria.

Minoxidil sulfate, a potent and ATP-sensitive K+ channel opener, is the sulfated metabolite of minoxidil. Minoxidil sulfate is considered as a vasodilator to promote hair growth in vivo.

Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC50 of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion.

Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al.

Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure.

DIMBOA, an antibiotic, is a benzoxazinoid, part of the chemical defense system of graminaceous plants such as maize, wheat, and rye. DIMBOA possess growth inhibitory properties against many strains of studied bacteria and fungi, such as Staphylococcus aureus, Escherichia coli as well as against Saccharomyces cerevisiae. DIMBOA exhibits a potent free-radical scavenging activity and a weaker iron (III) ions reducing activity. Antioxidant activity.

HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.

FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.

FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.

α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 subunit-containing nicotinic receptors (IC50 = 0.5 - 3.5 nM at α3β2 expressed in Xenopus oocytes). Also potently blocks β3-containing neuronal nicotinic receptors. Displays > 200-fold selectivity for α3β2 over α2β2, α4β2 and α3β4.

Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.

WL47 is a selective, high-affinity, disrupter of cavolin-1 oligomers (Kd=23 nM) than BSA, casein, and HEWL. WL47 is a caveolin-1 (CAV1) ligand and is 80% smaller in length than the original T20 parent sequence. WL47 can be used for the study of caveolin-1 function.

TfR-T12 is a BBB-penetrated transferrin receptor (TfR) binding peptide, displaying a binding affinity in the nM range[1][2].

Protein E7(43-62) is an E7-derived peptide with anti-tumor effects (short peptide spanning the 43th to 62th amino acid residues in the E7 protein).

Phenazine methylsulfate is a free radical generator. Phenazine methylsulfate has been used as an electron transfer reactant in cell viability assays. Phenazine methylsulfate induces ssDNA break formation in the presence of the reducing agent NADPH. Phenazine methylsulfate induces oxidative DNA damage in an alkaline comet assay and apoptosis.

2-Chloroacetamide is a preservative and is a herbicide for both uplands and paddy fields. 2-Chloroacetamide is a biocide in agriculture, glues, paints and coatings. 2-Chloroacetamide inhibits very-long-chain fatty acid elongase.

Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.

Gondoic acid (cis-11-Eicosenoic acid), a monounsaturated long-chain fatty acid, is contained in a variety of plant oils and nuts.

JFD01307SC is a glutamine synthetase inhibitor and anti-tuberculosis agent. JFD01307SC acts as a mimic of L-Glutamate and thus target enzymes involved in glutamine biosynthesis.

ICCB-19 inhibits RIPK1-dependent apoptosis (RDA) with IC50 of 2.01 μM.

5-Lipoxygenases (15-LO) inhibitor 1 is a heterocyclic pyrimidobenzothiazine compound that inhibits 15-LO with an IC50 value of 18 µM.

CBS-1117 is a novel fusion inhibitor with EC50 ∼3 μM against group 1 HA.

LDC195943(IMT1) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT).

LDC203974(IMT1B) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT) with improved pharmacokinetic profiles than LDC195943(IMT1).

CL2-SN-38 is a cleavable linker-based antibody-drug conjugate (ADC) containing the topoisomerase I inhibitor SN-38 and a maleimidocaproyl linker. CL2-SN-38 has been linked to tumor-selective human monoclonal antibodies, such as anti-CEACAM5 (hMN-14) to target SN-38 to tumor sites and improve its solubility. CL2-SN-38 linked to hMN-14 binds (Kd = 1.4 nM) and is cytotoxic to LoVo human colon adenocarcinoma cells (IC50 = 5.3 nM). CL2-SN-38 linked to hMN-14 increases survival in a colon carcinoma mouse model of lung metastasis.

DGY-06-116 is an irreversible covalent, selective Src inhibitor.

Finasteride Carboxaldehyde is a metabolite of Finasteride in human bile (M2 metabolite).

GR 125,743 is a novel 5-HT1B/1D receptor antagonist.

Diphenylterazine (DTZ) is a bioluminescence agent. Diphenylterazine alone yielded very little background, leading to excellent signal-to-background ratios.

JC-1 is a membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis.

Homo-PROTAC cereblon degrader 1, is a cereblon degrader.

Fmoc-Val-Ala-PAB-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Enantiomer of Entecavir

Eleutheroside D is an active lignan isolated from the root of Eleutherococcus senticosus, has anti-inflammatory and hypoglycemic activities. Eleutheroside D is an optical isomer of Eleutheroside E.

Reuterin is a broad-spectrum antimicrobial agent active against Gram positive and Gram negative bacteria, as well as yeasts, moulds and protozoa. Reuterin is produced by specific strains of Lactobacillus reuteri during anaerobic metabolism of glycerol. Reuterin also demonstrates potent antimicrobial activity against a broad panel of human and poultry meat campylobacter spp. Isolates.

APG-1387, a bivalent SMAC mimetic, is an IAP antagonist that can induce proteasomal degradation of IAPs. APG-1387 sensitizes immune-mediated cell apoptosis in cancers. APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.

DENV-IN-2 is a potent dengue viral replication extracted from patent WO2018215315A1, compound 6AB, has an EC50 of 0.016 nM. DENV-IN-2 shows high potent activity against all four serotypes of the Dengue virus with EC50s ranging from 0.013 to 0.029 nM.

Vc-MMAD consists the ADCs linker (Val-Cit) and potent tubulin (MMAD). Vc-MMAD is a drug-linker conjugate for ADC.

GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620

EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.

EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain.

Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.

POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis.

NCGC00092410 is a potent, selective, and nonsugar glucocerebrosidase (GC), with an IC50 of 31 nM. NCGC00092410 shows no activity against the related hydrolases at concentrations up to 77 μM. NCGC00092410 is a GC chaperone and increases the activity and lysosomal localization of glucocerebrosidase in mutant cell lines. NCGC00092410 can be used for the research of Gaucher disease.

Dasatinib metabolite M6 (Dasatinib carboxylic acid) is an oxidative metabolite of Dasatinib. Dasatinib is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase.

MLT-231 is a potent, highly selective allosteric MALT1 with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.

NF-κΒ activator 1 is a potent NF-κΒ activator with an EC50 of 0.9 μM. NF-κΒ activator 1 induces superoxide dismutase (SOD) 2 mRNA expression.

BAP9THP is a synthetic cytokinin derivative and a growth regulator. BAP9THP promotes chlorophyll retention (and senescence delay) in plant tissues exceptionally strongly, and growth of tobacco callus almost as strongly as 6-Benzylaminopurine (BAP). BAP9THP induces adventitious shoot formation ignificantly more strongly than N6-isopentenyladenine or Kinetin.

WL47 TFA is a selective, high-affinity, disrupter of cavolin-1 oligomers (Kd=23 nM) than BSA, casein, and HEWL. WL47 TFA is a caveolin-1 (CAV1) ligand and is 80% smaller in length than the original T20 parent sequence. WL47 TFA can be used for the study of caveolin-1 function.

Zandelisib is a phosphatidylinositol 3-kinase (PI3K) extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic.

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

ERK-IN-3 is a potent and oral of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.

Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib can be used for the research of multiple sclerosis (MS).

CPL304110 is a potent, orally active and selective of fibroblast growth factor receptors FGFR (1-3), with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively.

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer.

LC-2 is a potent and first-in-class degrader of endogenous KRAS G12C with DC50 values between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.

Fmoc-Gly-Gly-Phe-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist.

Treosulfan (NSC 39069, Treosulphan) is an alkylating agent used for conventional and high-dose chemotherapy regimens. Treosulfan is potently cytotoxic against pancreatic cancer cell lines.

Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER+ HER2-advanced breast cancer.

BMS-986144 is a third-generation, pan-genotype (GT) NS3/4A protease. BMS-986144 inhibits HCV replicon with EC50s of 2.3, 0.7, 1.0, 12, 8.0, and 5.8 nM for GT-1a, GT-1b, GT-2a, GT-3a, 1a R155X, and 1b D168V, respectively. BMS-986144 has the potential for the research of HCV infection.

CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.

Sodium oleate (Oleic acid sodium) is an abundant monounsaturated fatty acid sodium. Sodium oleate is a Na+/K+ ATPase activator.

Fosravuconazole L-lysine ethanolate (BMS-379224 L-lysine ethanolate), a prodrug of Ravuconazole, is an orally active broad spectrum antifungal agent. Fosravuconazole L-lysine ethanolate can be used for candidiasis, onychomycosis and parasitemia research.

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.

CU115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU 115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.

MBCQ is a potent and selective the type V phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ has IC50s >100 µM for PDE1, PDE2, PDE3, and PDE4, respectively. MBCQ dilates coronary arteries via potent and specific inhibition of cGMP-PDE.

YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.

4-APC hydrobromide is a highly sensitive and selective derivatization agent for aldehydes. 4-APC hydrobromide possesses an aniline moiety for a fast selective reaction with aliphatic aldehydes as well as a quaternary ammonium group for improved MS sensitivity. 4-APC hydrobromide allows highly sensitive and selective MS detection of aldehydes.

ALC-0315 is an ionisable aminolipid that used for mRNA compaction and aids mRNA cellular delivery. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles.

Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies.

Glutaminase-IN-3 (compound 657) is a potent glutaminase inhibitor extracted from patent WO2014089048A1, compound 657, has an IC50 of 0.24 μM for Glutaminase 1 (GLS1).

Novel lipid-lowering agent, acting as an AMPK activator, increasing ABCA1 protein expression and improving hepatic lipid metabolism and leukocyte trafficking in experimental hepatic steatosis

Novel SIRT6 activator, significantly inhibiting the proliferation and migration of pancreatic ductal adenocarcinoma (PDAC) cells in vitro and markedly suppressing the tumor growth in a PDAC tumor xenograft model

ARN-21934 is a novel potent and highly selective inhibitor for human topoisomerase II α over β.

Novel potent and selective NADPH oxidase inhibitor, targeting Nox4 in TGFβ-induced lens epithelial to mesenchymal transition

Novel mucolipin 1 (ML1) agonist, inducing lysosomal Ca2+ release, ameliorating muscular dystrophies and activating TFEB to correct lysosomal insufficiency in mdx mice

Hydrophobic inducer of the degradation of stabilized proteins, degrading HaloTag2 fusion proteins

SSAA09E2 is a novel inhibitor of SARS-CoV replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2)

Novel potent inhibitor of the GRK2--​dependent bovine tubulin oxidation

B3C is an activator of transcription factor MEF2D; Enhabcer of cognitive capacity; Blocker of N-methyl-D-aspartate receptors.

Novel inhibitor of SARS-CoV replication, acting by preventing fusion of the viral membrane with the host cellular membrane

Novel VISTA (V-domain immunoglobulin suppressor of T-cell activation) agonist

Novel covalent antagonist of hsSTING

Novel VISTA (V-domain immunoglobulin suppressor of T-cell activation) agonist

Potent and specific pan-PIM inhibitor, inhibiting proliferation of several AML cell lines, showing dual antitumoral and bone antiresorptive effects

Novel Potent Allosteric Activator for Ferroptosis Regulator Glutathione Peroxidase 4 (GPX4)

IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR. IFN alpha-IFNAR-IN-1 hydrochloride inhibits modified Vaccinia virus ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3- L-differentiated pDC cultures (BM-pDCs) (IC50=2-8 μM).

The first-in-class dual inhibitor of ENL (Kd = 754 ± 45 nM) and its paralog AF9 (Kd = 523 ± 53 nM)

Novel DNA polymerase inhibitor, inhibiting DNA replication in assays to assess global DNA synthesis or single-molecule bases by DNA fiber fluorography

Wu-5 is a USP10 inhibitor that can inhibit FLT3 and AMPK pathways, induce FLT3-ITD degradation and induce apoptosis.

Novel inhibitor of MuRF1, attenuating skeletal muscle atrophy and dysfunction in cardiac cachexia

Furimazine is an imidazopyrazinone substrate. NanoLuc (Nluc) paired with Furimazine produced 2.5 million-fold brighter luminescence in mammalian cells relative to Oluc-19 with Coelenterazine.

Novel fluorescent substrate for both the serotonin transporter and the vesicular monoamine transporter 2 (VMAT2)

RO6806051 (compound12) is a potent dual fatty acid binding protein 4 and 5 (FABP4 and FABP5) inhibitor with good selectivity and absorption, distribution, metabolism and excretion (eADME) properties.

Novel TDP-43 ligand, binding to TDP-43's RRM1 and RRM2 domains, partially disrupting TDP-43's interaction with the hexanucleotide RNA repeat of the disease-linked c9orf72 gene, improving larval turning, an assay measuring neuromuscular coordination and st

Novel modulator of Hydra head regeneration, inducing a homeotic transformation in Hydra

Novel selective uncompetitive inhibitor of DNA ligase I (LigI)

Novel autophagy inhibitor, selectively targeting cholesterol transfer protein GRAM domain-containing protein 1A (GRAMD1A), and directly competing with cholesterol binding to the GRAMD1A StART domain

DPI-201-106 is a cardioselective inhibitor of the TTX-resistant h1 Na channel inactivation. DPI-201-106 inhibits the L-type calcium current, and inward and delayed rectifier potassium currents.

Highly specific allosteric activator for the tumor-specific isoform of human pyruvate kinase M2 isoform (PKM2)

Novel Selective Histone Deacetylase 6 (HDAC6) Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

Natural inducer of apoptosis via Akt/NF-κB signaling suppression

Novel potent agonist of HTL/KAI2, stimulating activity for Arabidopsis seed germination

ML-179 is a potent inverse agonist of liver receptor homolog-1 (LRH-1) (IC50 = 320 nM) with maximum efficacy of 40% repression.

Selective blocker of the Aquaporin-1 ion channel conductance, slowing cancer cell migration

CRT5 is a pyrazine benzamide that prevents activation of all three isoforms of PKD in endothelial cells treated with VEGF (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively).

BMS 191011 is an activator of large-conductance calcium-activated potassium (BKCa) channels that increases maximum potassium current to 126% of control in X. laevis oocytes expressing human BKCa channels when used at a concentration of 1 μM.

Novel inhibitor of lactate dehydrogenase

Topical nonsteroidal antiandrogen (NSAA)

Novel FABP4/5 inhibitor, inhibiting lipolysis in 3T3-L1 adipocytes and in primary human adipocytes

Novel enhancer of endothelial NO synthase (eNOS)

Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes alpha-synuclein protein (IC50=1.5 uM). Synucleozid selectively targets the alpha-synuclein mRNA 5? UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson's disease[1]. IC50 & Target: IC50: 1.5 uM (SNCA IRE RNA)[1] In Vitro: Synucleozid (0.25-1 uM; 24 hours) abrogates cytotoxicity induced by alpha-synuclein preformed fibrils, which act as seeds and recruit endogenous alpha-synuclein to aggregate[1]. Synucleozid (0-1 uM; 24 hours) binds to the A bulge near the base of the IRE hairpin, reduced levels of alpha-synuclein in a dose-dependent manner with an IC50 of 500 nM, and inhibits alpha-synuclein protein expression in SH-SY5Y neuroblastoma cells[1]. Synucleozid (100 nM-100 uM; 24 hours) binds to 2-AP-labeled and native IRE RNA with similar affinities. It decreases 2-AP emission with an EC50 value of 2.7 uM, recovery of 2-AP emissions is observed as a function of unlabeled SNCA IRE RNA (RNA-0) concentration, affording a competitive Kd of 1.5 uM[1]. Synucleozid (0.25-1 uM; 24 hours) decreases alpha-synuclein and other proteins that have IREs in their mRNA's UTR including APP, PrP, Ferritin and TfR as a dose-dependent mannner. All panels is completed in SH-SY5Y cells, except for PrP protein which is assessed in Neuro-2A cells[1].

Novel potent SIRT6 activator against whole histone substrate

RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.

MGH-CP1 is a potent and selective TEAD palmitoylation inhibitor.

Novel upregulator of TRIB1 expression, leading to reprogramming of hepatic lipoprotein metabolism from lipogenesis to scavenging

Novel inhibitor of plasminogen activator inhibitor type 1 (PAI-1)

Potent and specific liver X receptor (LXR) dual agonist of LXRalpha and LXRbeta

F5446 is a SUV39H1 inhibitor. F5446 has an EC50 of 0.496 μmol/L for SUV39H1 enzymatic activity. H3K9me3 was enriched in the promoters of GZMB, PRF1, FASLG, and IFNG in quiescent T cells. F5446 inhibited H3K9me3, thereby upregulating expression of these effectors in tumor-infiltrating CTLs and suppressing colon carcinoma growth in a CD8+ CTL-dependent manner in vivo. Our data indicate that SUV39H1 represses CTL effector gene expression and, in doing so, confers colon cancer immune escape.

Potent aryl hydrocarbon receptor (AhR) ligand

Potent, orally active and S1P3-sparing S1P1 agonist

BMS-8 inhibits the PD-1/PD-L1 interaction with IC50 of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1[1].

SR 16584 is a selective antagonist of α3β4 nAChR with an IC50 of 10.2 μM.

G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory.

G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity.

NCGC2955 is a Novel Inhibitor of Human Cytomegalovirus (HCMV)

Novel 37/67kDa laminin receptor (LR) inhibitor, affecting both the direct 37/67kDa LR-PrP(C) interaction in vitro and the formation of the immunocomplex in live cells, inducing a progressive internalization of 37/67kDa LR and stabilization of PrP(C) on th

Novel potent and selective RIP3 kinase inhibitor

Dual inhibitor for lysophospholipase 1 (LYPLA1) and lysophospholipase 2 (LYPLA2)

Novel Potent Inhibitor of the Protein Phosphatase Slingshot

Novel pendrin inhibitor, attenuating airway hyperresponsiveness and mucin expression in experimental murine asthma

SP-13786(UAMC-1110) is a Novel potent and selective inhibitor of fibroblast activation protein (FAP), displaying low nanomolar inhibitory potency and high selectivity against the related dipeptidyl peptidases (DPPs) DPPIV, DPP9, DPPII, and prolyl oligopeptidase (PREP)

A sphingosine 1-phosphate (S1PR) receptor agonist

Novel suppressor of plant immune responses

Novel potent FKBP12 ligand

Novel potent and cell-active PARG inhibitor, selectively killing BRCA-mutant and PARP inhibitor-resistant cancer cells

Novel potent and selective antagonist of human Complement C3a receptor

Novel inhibitor of PKM2-regulated signaling, suppressing non-glycolytic PKM2-regulated signaling in cancer cells

AZ617 is a potent TLR4 agonist.

BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus T

HaloPROTAC3 is a degrader of HaloTag fusion proteins.

Novel FAK activator, promoting human intestinal epithelial monolayer wound closure and mouse ulcer healing

Novel antibiotic against a unique tRNA-mediated regulation of transcription in Gram-positive bacteria, significantly inhibiting in vivo transcription of glycyl-tRNA synthetase mRNA, also inhibiting in vivo translation of the S. aureus threonyl-tRNA synthe

Novel Inhibitor of StearoylCoA Desaturase-1 (SCD1)

6R-FR054 is a 6R-isomer of FR054. FR054 is an inhibitor of the Hexosamine Biosynthetic Pathway (HBP) enzyme PGM3, with a remarkable anti-breast cancer effect.

CGS-15943| is a highly potent, non-selective adenosine receptor antagonist.

CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers. CYM51010 exhibits anti-nociceptive activity similar to morphine, but with a decreased levels of tolerance development and withdrawal symptoms.

Aurachin D is an antibiotic. Aurachin D inhibits Gram-positive bacteria and a few funguses. Aurachin D blocks NADH oxidation in beef heart submitochondrial particles.

UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines[1]. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli[2].

Propargylcholine bromide is a choline analogue containing terminal propargyl that can be incorporated into all classes of Choline-containing phospholipids such as phosphatidylcholine and sphingomyelin, labeling Choline-containing phospholipids. Propargylcholine bromide-labeled phospholipid molecules can be visualized in cells with high sensitivity and spatial resolution.

4-Allylcatechol (4-Allylpyrocatechol, Hydroxychavicol) is an intermediate to synthetic safrole.

Inhibitor of placental alkaline phosphatase (PLAP)

Potent and selective EP4 antagonist

GSK1059865 is a potent orexin 1 receptor antagonist.

Potent hSirt3 Inhibitor

A potent and selective Adenosine receptor A2A agonist

HDAC-IN-4 is a selective HDAC6 and HDAC10 inhibitor with pIC50s of 7.2 and 6.8 in BRET assay, respectively. Antitumoral activity.

GalR2-positive allosteric modulator

Potent mGluR5 PAM modulator

VMAT2 ligand, stimulating dopamine release, inhibiting the reuptake of dopamine and serotonin, acting as a mixed agonist-antagonist at nicotinic acetylcholine receptors and antagonist at µ-opioid receptors

ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively.

Novel Orally Available Polymerase Inhibitor, Showing Efficacy Against a Lethal Morbillivirus Infection in a Large Animal Model

Novel glucocerebrosidase activator; Non-inhibitory chaperones of glucocerebrosidase

Novel Inhibitor of Monoubiquitinated Proliferating Cell Nuclear Antigen (PCNA), inhibiting Repair of Interstrand DNA Crosslink, enhancing DNA Double-strand Break, and sensitizing Cancer Cells to Cisplatin.

Novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe

9-Hydroxycanthin-6-one is an alkaloid compound. 9,10-Dimethoxycanthin-6-one exhibits NF-κB inhibitory effects with an IC50 of 3.8 μM.

RY785 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with an IC50 of 0.05 μM for KV2.2. RY785 has analgesic activity[1].

Potent, allosteric GPR55 antagonist

First reported nonpeptidomimetic agonist on the G protein-coupled chemokine receptor CXCR-3

Novel Multitarget Modulator of Alzheimer's Disease

Antagonist for G-protein Coupled Receptor 7 (GPR7)

Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction

Competitive inhibitor of secretory phospholipase A2 (sPLA2)

Novel allosteric agonist of Sphingosine 1-phosphate receptor 2 (S1PR2)

First-in-class Haspin inhibitor with a wide spectrum of anticancer effects

Novel glucocerebrosidase activator; Non-inhibitory chaperones of glucocerebrosidase

Unique F-box/LRR-repeat protein 2 (FBXL2) activator

GABA-A modulator, blocking the sedative effects without lowering the convulsion threshold

Potent and selective blocker for TMEM16A/Anoctamin-1 (ANO1)

Novel dopamine D3 receptor-selective partial agonist

Selective RIP3 kinase inhibitor

Novel selective PAD4 inhibitor

GSK106 is a negative control compound used in binding and functional assays for PAD4 inhibitors.

Novel Potent and Selective Positive Allosteric Modulators of the delta-Opioid Recepto

FIPI (5-Fluoro-2-indolyl des-chlorohalopemide) hydrochloride, a derivative of Halopemide (HY-119093), is a phospholipase D (PLD) inhibitor with IC50s of approximately 25 nM and 20 nM for PLD1 and PLD2, respectively. FIPI hydrochloride inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. FIPI hydrochloride has the potential for autoimmunity and cancer metastasis research.

Selective 5-HT1B serotonin receptor antagonist

A potent and selective inhibitor of mitochondrial Na+/Ca2+ exchanger mNCX with neuroprotective activity. It was shown to reduce Ca2+ efflux from the mitochondria to the cytosol with an EC50 value of 690 nM and was shown to protect against Ca2+ overload an

Novel selective inhibitor of collagen prolyl 4-hydroxylase, neither causing general toxicity nor disrupting iron homeostasis

SGC2085 is a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo.

Novel proteasome inhibitor, inducing human myeloid tumor-selective apoptosis

Cytokine release inhibitor, inhibiting production of IL-1ß, IL-8, IL-6, IL-10 and TNFalpha

Negative control for GSK'963 (AOB9775). Novel highly potent and selective RIP1 inhibitor

Novel modulator of the UNC119-Cargo Interaction, potently and selectively inhibiting the binding of a myristoylated peptide representing the N-terminus of Src kinase to UNC119A

Selective estrogen receptor modulator (SERM), inhibiting mammalian PLD (PLD1 and PLD2)

Sultopride hydrochloride (LIN-1418 hydrochloride) is a selective antagonist of dopamine D2 receptor.

Neutral retinoic acid receptor (RAR) α-selective antagonist