GSK25

GSK25 is an inhibitor of Rho-associated kinase 1 (ROCK1, IC50 = 7 nM for the human kinase). It is selective for ROCK1 over p90 ribosomal S6 kinase 1 (RSK1) and p70 ribosomal S6 kinase (p70S6K, IC50s = 398 and 1,000 nM, respectively) and is greater than 100-fold selective over a panel of 31 additional kinases. GSK25 induces relaxation in precontracted isolated rat aortic rings (EC50 = 256 nM). In vivo, GSK25 (30 mg/kg) decreases mean arterial blood pressure in spontaneously hypertensive rats.Formal Name: 4-(4-chloro-2-fluorophenyl)-2-(2-chloro-4-pyridinyl)-N-(6-fluoro-1H-indazol-5-yl)-1,4-dihydro-6-methyl-5-pyrimidinecarboxamide. CAS Number: 874119-56-9. Molecular Formula: C24H16Cl2F2N6O. Formula Weight: 513.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 10 mg/ml. SMILES: O=C(C1=C(C)N=C(C2=CC(Cl)=NC=C2)N[C@@H]1C3=CC=C(C=C3F)Cl)NC4=CC5=C(C=C4F)NN=C5. InChi Code: InChI=1S/C24H16Cl2F2N6O/c1-11-21(24(35)32-19-6-13-10-30-34-18(13)9-17(19)28)22(15-3-2-14(25)8-16(15)27)33-23(31-11)12-4-5-29-20(26)7-12/h2-10,22H,1H3,(H,30,34)(H,31,33)(H,32,35)/t22-/m1/s1. InChi Key: KZYAHEIPPAPADQ-JOCHJYFZSA-N.