Novel PDZ binding kinase (PBK) inhibitor.

S isomer of R-Etomoxir

Cephalosporin C Na salt is used to study the effect of transpeptidase expression, binding, and inhibition on bacterial cell wall mucopeptide synthesis.

DL-AP5 is a Broad spectrum EAA antagonist.

Nicotinamide riboside, also known as NR and SRT647, is a pyridine-nucleoside form of vitamin B3 that functions as a precursor to nicotinamide adenine dinucleotide or NAD+. NR blocks degeneration of surgically severed dorsal root ganglion neurons ex vivo and protects against noise-induced hearing loss in living mice. Nicotinamide riboside prevents muscle, neural and melanocyte stem cell senescence. Increased muscular regeneration in mice has been observed after treatment with nicotinamide riboside, leading to speculation that it might improve regeneration of organs such as the liver, kidney, and heart. Nicotinamide riboside also lowers blood glucose and fatty liver in prediabetic and type 2 diabetic models while preventing the development of diabetic peripheral neuropathy. Note: Nicotinamide Riboside chloride is a α/β mixture

AY-NH2 is a peptide agonist of proteinase-activated receptor 4 (PAR4) that induces aggregation of rat and human platelets in vitro (EC50s = 15 and 60 μM, respectively).

Arg-Gly-Asp-Ser(RGDS peptide) is an integrin binding sequence that inhibits integrin receptor function; decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS

Dnp-PLG-Cys(Me)-HA-DArg-NH2 is a peptide substrate for matrix metalloproteinase-1 (MMP-1).It has an improved kcat/Km ratio compared with the MMP-1 flurogenic substrate Dnp-PLGLWA-DArg-NH2.

MMP-3 inhibitor is a peptide inhibitor of matrix metalloproteinase-3 (MMP-3) with a Ki value of 95 nM.

AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM. AS105 is also effective against autophosphorylated CaMKII (in contrast to the commonly used allosteric CaMKII-inhibitor KN-93). In isolated atrial cardiomyocytes from human donors and ventricular myocytes from CaMKIIδC-overexpressing mice with heart failure, AS105 effectively reduced diastolic SR Ca2+ leak by 38% to 65% as measured by Ca2+-sparks or tetracaine-sensitive shift in [Ca2+]i. AS105 effectively reduced SR Ca2+-leak, thus improving SR Ca2+-accumulation and reducing cellular arrhythmogenic correlates, without negatively influencing excitation-contraction coupling.

MS.001 is a small molecule that inhibits both the chaperone binding and ubiquitin ligase activity of C-terminus of Hsc70 interacting protein (CHIP) at low micromolar concentrations (IC50=3.3 uM).

DCC-3116 (DCC3116) is a first-in-class, selective inhibitor of ULK1/2 kinases (IC50=4.7/35 nM) and autophagy.DCC-3116 is an oral ULK1/2 inhibitor targeting the autophagy pathway, a key mechanism of tumor survival and resistance to targeted therapy.

Diloxanide furoate is an ambecide, an anti-protozoal drug used in the treatment of amoebozoa infections

SBI-425 (SBI425) is a potent, selective, orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor with IC50 of 16 nM, shows high selectivity over other alkaline phosphatases including IAP and PLAP.

Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.

Ribavirin carboxylic acid (TR-COOH) is a metabolite of ribavirin, ribavirin has strong antiviral activity.

BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.

Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor.

LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.

GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA.

NNC 05-2090 is a potent selective GABA transporter inhibitor of mGAT2 with Ki of 1.4 uM.

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.

MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity.

BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.

A potent, specific, allosteric inhibitor of KSP motor domain ATPase with Ki of 12 nM.

SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells.

ZINC00640089 is a specific Lipocalin-2 (LCN2) inhibitor. ZINC00640089 inhibits cell proliferation, cell viability and reduces AKT phosphorylation levels in SUM149 cells. ZINC00640089 has good potential for research in inflammatory breast cancer (IBC).

A potent tyrosine kinases inhibitor with IC50 of 13/9/3/26/2 nM for Lck/Btk/Lyn/Syk/Txk..

MIND4-19 is a potent SIRT2 inhibitor with an IC50 value of 7.0 μM. MIND4-19 can be used for researching Huntington's disease.

Sirtuin modulator 2 (Compound 132) is a sirtuin modulator with an ED50 equal or less than 50 μM.