H-1152
Cat. No.：YN290778
| 产品名称: | H-1152 |
| CAS No.: | 451462-58-1 |
| Chemical Name: | 5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-4-methyl-isoquinoline, dihydrochloride |
| Synonyms: | H 1152;H1152 |
| 分子量: | 392.3 |
| 分子式: | C16H21N3O2S • 2HCl |
| SMILES: | CC1=CN=CC2=C1C(S(N3CCCNC[C@@H]3C)(=O)=O)=CC=C2.Cl.Cl |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | H-1152 是一种膜通透的，选择性的ROCK抑制剂，Ki值为 1.6 nM，对ROCK2的IC50值为 12 nM。 |
| IC50和靶点: | [{name:"ROCKII:12 nM (IC50)"},{name: "PKA:3.03 μM (IC50)"},{name: "PKC:5.68 μM (IC50)"},{name: "PKG:0.36 μM (IC50)"},{name: "MLCK:28.3 μM (IC50)"},{name: "CaMKII:0.18 μM (IC50)"},{name: "AuroraA:0.745 μM (IC50)"},{name: "GSK3α:60.7 μM (IC50)"},{name: "AMPK:100 μM (IC50)"},{name: "P38α:100 μM (IC50)"},{name: "MKK4:16.9 μM (IC50)"},{name: "Abl:7.77 μM (IC50)"},{name: "Src:3.06 μM (IC50)"},{name: "EGFR:50 μM (IC50)"}] |
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Sasaki, Y., Suzuki, M., and Hidaka, H.The novel and specific Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinoline)sulfonyl]-homopiperazine as a probing molecule for Rho-kinase-involved pathwayPharmacol. Ther.93,225-232(2002)
Ikenoya, M., Hidaka, H., Hosoya, T., 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 inhibitorJ. Neurochem.81,9-16(2002)
Davies, S.L., Gibbons, C.E., Vizard, T., et al.Ca2+-sensing receptor induces Rho kinase-mediated actin stress fiber assembly and altered cell morphology, but not in response to aromatic amino acidsAm. J. Physiol. Cell Physiol.290,C1543-C1551(2006)
Johnson, R.P., El-Yazbi, A.F., Takeya, K., et al.Ca2+ sensitization via phosphorylation of myosin phosphatase targeting subunit at threonine-855 by Rho kinase contributes to the arterial myogenic responseJ. Physiol.587(11),2537-2553(2009)
Rattan, S., and Patel, C.A.Selectivity of Rho kinase (ROCK) inhibitors in the spontaneously tonic smooth muscleAm. J. Physiol. Gastrointest. Liver Physiol.294(3),G687-G693(2008)
Fuentes, E.O., Leemhuis, J., Stark, G.B., et al.Rho kinase inhibitors Y27632 and H1152 augment neurite extension in the presence of cultured Schwann cellsJ. Brachial Plex. Peripher. Nerve Inj.3(19),(2008)
