GSK429286A

• CAT Number: I005189
• CAS Number: 864082-47-3
• Molecular Formula: C₂₁H₁₆F₄N₄O₂
• Molecular Weight: 432.27
• Purity: ≥95%
• Synonyms: N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide
• Target: TGF-beta/Smad
• Solubility: DMSO: ≥ 51 mg/mL
• Storage: 2-8°C
• IC50: 14 nM(ROCK1); 63 nM(ROCK2)
• InChI: InChI=1S/C21H16F4N4O2/c1-10-19(20(31)28-17-6-12-9-26-29-16(12)8-15(17)22)14(7-18(30)27-10)11-2-4-13(5-3-11)21(23,24)25/h2-6,8-9,14H,7H2,1H3,(H,26,29)(H,27,30)(H,28,31)
• InChIKey: OLIIUAHHAZEXEX-UHFFFAOYSA-N
• SMILES: CC1=C(C(CC(=O)N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NC3=C(C=C4C(=C3)C=NN4)F

GSK429286A is a potent and selective inhibitor of ROCK1 and ROCK2, with IC50 values of 14 nM and 63 nM, respectively. Optimizing the use of this inhibitor could lead to potential therapeutic applications in various diseases such as cancer, cardiovascular disease, and neurological disorders.

Reference

[1]. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9.
[2]. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson/’s disease. Biochem J. 2009 Oct 23;424(1):47-60.