Hydroxyfasudil

• CAT Number: I000291
• CAS Number: 105628-72-6
• Molecular Formula: C14H17N3O3S
• Molecular Weight: 307.37
• Purity: ≥95%
• Synonyms: 5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one
• Target: ROCK
• Solubility: DMSO: ≥ 31 mg/mL
• Storage: Store at -20°C
• IC50: 0.12 uM (ROCK1); 0.17 uM (ROCK2)
• InChI: InChI=1S/C14H17N3O3S/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19,20)17-9-2-6-15-8-10-17/h1,3-5,7,15H,2,6,8-10H2,(H,16,18)
• InChIKey: ZAVGJDAFCZAWSZ-UHFFFAOYSA-N
• SMILES: C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O

Hydroxyfasudil（Cat No.:I000291） is a potent inhibitor of the Rho-associated protein kinases (ROCK1 and ROCK2), with IC50 values of 0.73 μM and 0.72 μM, respectively. As a ROCK inhibitor, it exerts its inhibitory effects on ROCK-mediated signaling pathways involved in cellular functions such as cell contraction, migration, and adhesion. Hydroxyfasudil has been investigated for its potential therapeutic applications in various diseases, including cardiovascular disorders, neurological disorders, and cancer. Its inhibitory activity against ROCK makes it a valuable tool for studying the roles of ROCK in cellular processes and for developing targeted therapies.

Reference

[1]. Tsutomu Akama, et al. Linking Phenotype to Kinase: Identification of a Novel Benzoxaborole Hinge Binding Motif for Kinase Inhibition and the Development of High Potency Rho-Kinase Inhibitors. JPET Fast Forward. Published on September 18, 2013.

[2]. Satoh S, et al. Evidence of a direct cellular protective effect of Rho-kinase inhibitors on endothelin-induced cardiac myocyte hypertrophy. Biochem Biophys Res Commun. 2012 Jul 27;424(2):338-40.

[3]. Shimizu N, et al. Effects of the Rho kinase inhibitor, hydroxyfasudil, on bladder dysfunction and inflammation in rats with HCl-induced cystitis. Int J Urol. 2013 Feb 19.

[4]. Saito M, et al. Hydroxyfasudil ameliorates penile dysfunction in the male spontaneously hypertensive rat. Pharmacol Res. 2012 Oct;66(4):325-31.

[5]. Zhao J, et al. Efficacy and safety of fasudil in patients with subarachnoid hemorrhage: final results of a randomized trial offasudil versus nimodipine. Neurol Med Chir (Tokyo). 2011;51(10):679-83.