Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
500 μg | 約 35 days | ¥ 53,500 |
1 mg | 約 35 days | ¥ 101,000 |
5 mg | 約 35 days | ¥ 418,000 |
10 mg | 約 35 days | ¥ 730,000 |
説明 | 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). |
ターゲット&IC50 | 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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PBS (pH 7.2): 10 mg/mL
DMSO: 10 mg/mL
Ethanol: 2 mg/mL
DMF: 5 mg/mL
You can also refer to dose conversion for different animals. 詳細
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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