| 货号 | 13332-10mg |
| 描述 | Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal.123 Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II).4 It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each).4 The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).4,5 |
| 别名 | Rho Kinase Inhibitor IV; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Olson, M.F. Applications for ROCK kinase inhibition. Current Opinion in Cell Biology 20, 242-248 (2008). 2.Narumiya, S.,Tanji, M., and Ishizaki, T. Rho signaling, ROCK and mDia1, in transformation, metastasis and invasion. Cancer Metastasis Reviews 28, 65-76 (2009). 3.Watanabe, K.,Ueno, M.,Kamiya, D., et al. A ROCK inhibitor permits survival of dissociated human embryonic stem cells. Nature Biotechnology 25(6), 681-686 (2007). 4.Tamura, M.,Nakao, H.,Yoshizaki, H., et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochimica et Biophysica Acta 1754, 245-252 (2005). 5.Ishizaki, T.,Uehata, M.,Tamechika, I., et al. Pharmacological properties of Y-27632, a specific inhibitor of Rho-associated kinases. Molecular Pharmacology 57, 976-983 (2000). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 449.4 |
| 分子式 | C18H24N4O3S • 2HCl |
| CAS号 | 913844-45-8 |
| 稳定性 | ≥ 2 years |
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