9 products were found matching "Cay13498-%25"!

GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1, IC50 = 0.5 nM). It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg. GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic...

Cyclophosphamide is a nitrogen mustard alkylating agent. It acts as a prodrug and is converted to the active metabolite phosphoramide mustard (Cay-34078) via 4-hydroxycyclophosphamide and aldophosphamide intermediates by cytochrome P450s (CYP450s) in the liver. Cyclophosphamide (50 mg/kg) induces the formation of...

13,14-dihydro-15-keto-Prostaglandin E2-d9 (13,14-dihydro-15-keto PGE2-d9) is intended for use as an internal standard for the quantification of 13,14-dihydro-15-keto PGE2 (Cay-14650) by GC- or LC-MS. 13,14-dihydro-15-keto PGE2 is a metabolite of PGE2 (Cay-14010) and the primary PGE2 metabolite in plasma. It is...

Glycopyrrolate is an antagonist of muscarinic acetylcholine receptors (mAChRs, Kis = 0.42, 1.77, 0.52, 0.78, and 1.29 nM for the M1-M5 receptors, respectively). It induces relaxation of precontracted isolated human bronchi when used at concentrations of 0.01, 0.1, or 1 µM. Glycopyrrolate reduces post-prandial...

HA-130 is a reversible inhibitor of autotaxin, completely blocking the hydrolysis of the substrate bis-pNPP with an IC50 value of 28 nM. It does not affect the activity of any proteasomal protease or related enzymes. HA-130 rapidly decreases plasma lysophosphatidic acid levels in mice when given intravenously (1...

Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Cay-81590). It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCalpha,...

Regorafenib is an orally bioavailable multi-kinase inhibitor with anticancer activity. It inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRbeta with IC50 values of 1.5, 2.5, 4.2, 7, 13, and 22 nM, respectively. Regorafenib also inhibits B-RAF, VEGFR3, FGFR, and Tie2 (IC50s = 28, 46, 202, and 311 nM, respectivey)...

The Src family of non-receptor tyrosine kinases regulate cell adhesion, growth, and differentiation through activation of multiple intracellular signaling pathways. Normally inactive, Src kinases are transiently activated during mitosis and constitutively activated by abnormal mutations. PP2 is a potent, reversible,...

MPI-0441138 is a potent inducer of apoptosis and growth inhibition (EC50 = 2 nM for both processes, based on caspase-3 activation and total cellular ATP, respectively) in T47D and HCT116 cells. MPI-0441138 has excellent blood brain barrier penetration and is effective in mouse xenograft cancer models.Formal Name:...