Vacquinol-1 dihydrochloride (also known as NSC-13316; NSC13316) is an MKK4 (mitogen-activated protein kinase kinase 4) activator with antitumor activity. It rapidly and selectively induces glioma cell death. Also inducing apoptosis in hepatocellular carcinoma (HCC)cell. Research showed that vacquinol-1 displayed high cytotoxicity against glioma cells, resulting in a complete loss of viability as measured by ATP […]

JTE 013 (JTE-013) is a novel potent and selective S1P2 (sphingosine-1-phosphate 2) antagonist with IC50 of 17.6 nM. It binds to the human and rat receptors with IC50 values of 17 and 22 nM, respectively, and with IC50 values >10 µM for human S1P1 and S1P3. It reverses the inhibitory effects of S1P2 signaling on […]

Voxelotor (formerly known as GBT-440; trade name: Oxbryta) is a potent and orally bioactive allosteric effector of sickle cell hemoglobin. It increases the affinity of hemoglobin for oxygen and consequently inhibits its polymerization when subjected to hypoxic conditions. Unlike earlier allosteric activators that bind covalently to hemoglobin in a 2:1 stoichiometry, Voxelotor binds with a […]

STO-609 acetate is a novel, potent, specific and cell-permeable inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms with Ki values of 80 and 15 ng/ml, respectively, it also inhibits their autophosphorylation activities. STO-609 inhibits the activities of recombinant CaM-KK alpha and CaM-KK beta isoforms, with K(i) […]

Verubecestat TFA (also known as MK-8931; SCH-900931), the trifluoroacetic acid salt form of MK-8931, is a beta-secretase 1 and BACE1 inhibitor with anti-AD (Alzheimer’s disease) activity. It is in Phase 3 clinical trial for treatment of Alzheimer’s disease. Amyloidogenic pathway in Alzheimer’s disease (AD) involves breakdown of APP by β-secretase followed by γ-secretase and results […]

CCT245737 S-enantiomer, the S-isomer of CCT-245737, is an orally available and selective ATP-competitive inhibitor of CHK1 (checkpoint kinase 1) with an IC50 of 30-220 nM.

Sivelestat (also known as ONO5046; LY544349; EI546) is a novel, potent and competitive inhibitor of human neutrophil elastase (HNE) with IC50 value of 44 nM and Ki of 200 nM; it also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse. ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and […]