H-1152 Dihydrochloride

CAS: 871543-07-6

Ref. TR-H011520

Product Information

• Name: H-1152 Dihydrochloride
• Synonyms: 4-methyl-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline;dihydrochloride

Description

Stability Hygroscopic
Applications ROCK Inhibitor. A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK: Ki=1.6nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki=630nM for PKA 9.27 mMfor PKC, and 10.1mM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50=2.5nM) in NT-2 cells.
References Ikenoya, M., et al.: J. Neurochem., 81, 9 (2002), Sasaki, Y., et al.: Pharmacol. Ther., 93, 225 (2002)

• Brand: TRC

Chemical properties

• Molecular weight: 392.34
• Formula: C₁₆H₂₁N₃O₂SClH
• Color/Form: Neat
• InChI: 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
• InChI key: InChIKey=AWDORCFLUJZUQS-ZDUSSCGKSA-N
• SMILES: Cc1cncc2cccc(S(=O)(=O)N3CCCNC[C@@H]3C)c12