Cayman Chemical | Glycyl-H-1152 (hydrochloride) | Description • Rho Kinase Inhibitor IV (CAS 913844-45-8)

13332 Glycyl-H-1152 (hydrochloride)

Rho Kinase Inhibitor IV (CAS 913844-45-8)

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Two Rho kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The Rho kinases 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 hydrochloride) and exhibits better specificity. Thus, it poorly inhibits calcium/calmodulin kinase II, protein kinase 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 (K_i = 220 nM) and HA-1077 (IC₅₀ = 158 nM).^4,5

1 Olson, M.F. Applications for ROCK kinase inhibition. Curr Opin Cell Biol 20 242-248 (2008).

2 Narumiya, S., Tanji, M., Ishizaki, T. Rho signaling, ROCK and mDia1, in transformation, metastasis and invasion. Cancer Metastasis Rev 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. Biochim Biophys 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. Mol Pharmacol 57 976-983 (2000).

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Pricing updated 2010-03-19.
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