应用 |
A cell permeable, highly specific, and potent ATP-competitive inhibitor of ρ-kinase inhibitor。 |
产品介绍 |
H-1152是特异的高活性Rho激酶抑制剂,可渗透入细胞膜,Ki为1.6 nM,对其它丝氨酸/苏氨酸激酶抑制性极低。 |
生化机理 |
H-1152 is a selective ATP-competitive inhibitor of rho-kinase (ROCK) inhibitor, cell permeable, highly specific, and potent (Ki = 1.6 nM). Exhibits weaker affinity for other serine/threonine kinases (Ki = 630 nM for PKA, 9.27mM for PKC and 10.1 mM for MLCK) and is more potent and selective than Y-27632. Inhibits the phosphorylation of MARCKS in cells stimulated by lysophosphatidic acid and inhibits EP3-stimulated NO formation. H-1152 . dihydrochloride prevents fragmentation of apoptotic cells. Relieves neuropathic pain. |
别名 |
H 1152;H1152;4-甲基-5-{[(2S)-2-甲基-1,4-二氮杂环庚-1-基]磺酰基}异喹啉;H 1152;H1152; 4-methyl-5-{[(2s)-2-methyl-1,4-diazepan-1-yl]sulfonyl}isoquinoline ;(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine |