Sorafenib (BAY 43-9006) Tosylate is an orally active multikinase inhibitor of tyrosine protein kinases VEGFR/PDGFR and RAF/MEK/ERK with IC50 values of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
KN-92 hydrochloride is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 hydrochloride is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93.
Acetohexamide is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2; stimulate the pancreas to secrete insulin.
YKL-5-124 is a potent, selective, irreversible COVALENT inhibitor of CDK7 and CDK7/Mat1/CycH IC50 53.5 nM and 9.7 nM, respectively. YKL-5-124 is more than 100 times more selective to CDK7 than CDK9 and CDK2 and is inactive to CDK12 and CDK13. YKL-5-124 induces intense cell cycle arrest and inhibits E2F-driven gene expression with little effect on RNA...
BMS-707035 is an HIV-1 integrase (IN) inhibitor. HIV-1 integrase (IN) represents a therapeutically advantageous viral target to treat HIV/AIDS in the clinic.
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia.
Navarixin (SCH 527123) is a novel, selective CXCR2 receptor antagonist with IC50 of 3 nM. Navarixin (SCH 527123) has Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P1 receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis).
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.
Mivebresib(ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4)
JPH203, a selective L-type amino acid transporter 1 (LAT1) inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leukemic cells.