KD 025

KD 025 is an inhibitor of Rho-associated kinase 2 (ROCK2, IC50 = 0.105 µM). It is selective for ROCK2 over ROCK1 (IC50 = 24 µM). KD 025 (10 µM) decreases the expression of connective tissue growth factor (CTGF) and induces remodeling of the actin cytoskeleton in isolated human ileal fibrotic smooth muscle cells. It inhibits heat-killed C. albicans- or S. epidermidis-induced production of IL-17 in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 1.25 to 10 µM. KD 025 (100 and 200 mg/kg) reduces infarct volume in a mouse model of cerebral ischemia induced by transient middle cerebral artery occlusion (MCAO). It decreases disease severity in a mouse model of sclerodermatous chronic graft versus host disease (GVHD) when administered at a dose of 150 mg/kg. Formulations containing KD 025 have been used in the treatment of chronic GVHD.Formal Name: 2-[3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy]-N-(1-methylethyl)-acetamide. CAS Number: 911417-87-3. Synonyms: Belumosudil, SLx-2119. Molecular Formula: C26H24N6O2. Formula Weight: 452.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 25 mg/ml. lambdamax: 248, 304, 338 nm. SMILES: O=C(NC(C)C)COC1=CC=CC(C2=NC3=CC=CC=C3C(NC4=CC(C=NN5)=C5C=C4)=N2)=C1. InChi Code: InChI=1S/C26H24N6O2/c1-16(2)28-24(33)15-34-20-7-5-6-17(13-20)25-30-23-9-4-3-8-21(23)26(31-25)29-19-10-11-22-18(12-19)14-27-32-22/h3-14,16H,15H2,1-2H3,(H,27,32)(H,28,33)(H,29,30,31). InChi Key: GKHIVNAUVKXIIY-UHFFFAOYSA-N.