| 货号 | 10007653-500ug |
| 描述 | Rho-associated kinase (ROCK), activated by GTP-linked Rho, phosphorylates targets that are involved in cytoskeletal remodeling, smooth muscle contraction, and neuronal development. H-1152 is a potent, specific, ATP-competitive, and cell permeable inhibitor of ROCK (Ki = 1.6 nM).12 It is a more potent inhibitor of ROCK than either Y-27632 (Ki = 140 nM) or HA-1077 (Ki = 330 nM).2 H-1152 poorly inhibits PKA, PKC, and myosin light chain kinase (Ki = 0.63, 9.27, and 10.1 μM, respectively).2 It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly,3vasoconstriction,4 as well as spontaneously tonic smooth muscle5 and neurite extension.6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.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 pathway. Pharmacology & Therapeutics 93, 225-232 (2002). 2.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 inhibitor. Journal of Neurochemistry 81, 9-16 (2002). 3.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 acids. American Journal of Physiology.Cell Physiology 290, C1543-C1551 (2006). 4.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 response. Journal of Physiology 587(11), 2537-2553 (2009). 5.Rattan, S., and Patel, C.A. Selectivity of Rho kinase (ROCK) inhibitors in the spontaneously tonic smooth muscle. American Journal of Physiology and Gastrointestinal Liver Physiology 294(3), G687-G693 (2008). 6.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 cells. Journal of Brachial Plexus and Peripheral Nerve Injury 3(19), (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 392.3 |
| 分子式 | C16H21N3O2S • 2HCl |
| CAS号 | 451462-58-1 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |