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Rho Kinase Inhibitor
H-1152, H-1152P, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine, 2HCl, ROCK Inhibitor, Dimethylfasudil (diMF, H-1152P)
A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki = 630 nM for PKA, 9.27 μM for PKC, and 10.1 μM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50 = 2.5 μM) in NT-2 cells. Reported to be more potent and selective than Y-27632 (Cat. Nos. 688000 and 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL). At 10 mM (500 µg/128 µl) solution of Rho Kinase Inhibitor (Cat. No. 555552) in H2O is also available.
产品信息
Form White solid
Primary Target ROCK
Primary Target Ki 1.6 nM
Secondary target Ki = 630 nM for PKA, 9.27 mM for PKC, and 10.1 mM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50 = 2.5 mM) in NT-2 cells
Molar mass 392.3
Protect from Light 是的
Hygrocopic 是的
Packaged under inert gas 是的
Cell permeable 是的
ATP Competitive 是的
Purity ≥95% by HPLC
Solubility H2O or MeOH
Chemical formula C16H21N3O2S • 2HCl
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Harmful |