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Glycyl H-1152 hydrochloride

Glycyl H-1152 hydrochloride

产品编号 T35459   CAS 913844-45-8

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. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). 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). 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).

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Glycyl H-1152 hydrochloride Chemical Structure
Glycyl H-1152 hydrochloride, CAS 913844-45-8
规格 价格/CNY 货期 数量
500 μg ¥ 1,620 35日内发货
1 mg ¥ 2,970 35日内发货
5 mg ¥ 12,700 35日内发货
10 mg ¥ 22,200 35日内发货
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产品目录号及名称: Glycyl H-1152 hydrochloride (T35459)
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产品描述 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. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). 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). 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).
靶点活性 Aurora A:2.35 μM (IC50), PKG:3.26 μM (IC50), ROCKII:11.8 nM (IC50), CaMK II:2.57 μM (IC50)
分子量 449.39
分子式 C18H26Cl2N4O3S
CAS No. 913844-45-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

PBS (pH 7.2): 10 mg/mL

DMSO: 10 mg/mL

Ethanol: 2 mg/mL

DMF: 5 mg/mL

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Keywords

Glycyl H-1152 hydrochloride 913844-45-8 Glycyl H-1152 Hydrochloride Glycyl H1152 Hydrochloride Glycyl H1152 hydrochloride Glycyl H 1152 Hydrochloride Glycyl H 1152 hydrochloride Inhibitor inhibitor inhibit

 

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