H-1152 dihydrochloride

• CAT Number: I005249
• CAS Number: 871543-07-6
• Molecular Formula: C16H23Cl2N3O2S
• Molecular Weight: 392.34
• Purity: ≥95%
• Synonyms: 4-methyl-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline dihydrochloride
• Target: TGF-beta/Smad
• Solubility: DMSO: ≥ 32 mg/mL
• Storage: Store at -20°C
• IC50: 1.6 nM (Ki Value) [1]
• IUPAC Name: 4-methyl-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline;dihydrochloride
• InChI: 1S/C16H21N3O2S.2ClH/c1-12-9-18-11-14-5-3-6-15(16(12)14)22(20,21)19-8-4-7-17-10-13(19)2;;/h3,5-6,9,11,13,17H,4,7-8,10H2,1-2H3;2*1H/t13-;;/m0../s1
• InChIKey: BFOPDSJOLUQULZ-GXKRWWSZSA-N
• SMILES: C[C@H]1CNCCCN1S(=O)(=O)C2=CC=CC3=C2C(=CN=C3)C.Cl.Cl

H-1152 dihydrochloride (Cat No.: I005249) is a potent and selective inhibitor of Rho-associated protein kinases (ROCK1 and ROCK2), key regulators of cytoskeletal dynamics, cell motility, and vascular tone. By inhibiting ROCK activity, H-1152 modulates smooth muscle contraction, neuronal signaling, and inflammatory responses. It is widely used in research on cardiovascular diseases, neurodegeneration, cancer, and glaucoma. Its high potency and selectivity make it a valuable tool for dissecting Rho/ROCK signaling pathways and exploring therapeutic strategies targeting cytoskeletal remodeling and related pathological conditions.

Reference

[1]. Ikenoya M, et al. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16.
[2]. Teixeira CE, et al. Proerectile effects of the Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine (H-1152) in the rat penis. J Pharmacol Exp Ther. 2005 Oct;315(1):155-62.
[3]. Kroll J, et al. Inhibition of Rho-dependent kinases ROCK I/II activates VEGF-driven retinal neovascularization and sprouting angiogenesis. Am J Physiol Heart Circ Physiol. 2009 Mar;296(3):H893-9.
[4]. Yu M, et al. H-1152 effects on intraocular pressure and trabecular meshwork morphology of rat eyes. J Ocul Pharmacol Ther. 2008 Aug;24(4):373-9.