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Pack Size | Price | Availability | Quantity |
---|---|---|---|
500 μg | $233 | 35 days | |
1 mg | $440 | 35 days | |
5 mg | $1,820 | 35 days | |
10 mg | $3,180 | 35 days |
Description | 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). |
Targets&IC50 | Aurora A:2.35 μM (IC50), PKG:3.26 μM (IC50), CaMK II:2.57 μM (IC50), ROCKII:11.8 nM (IC50) |
Molecular Weight | 449.39 |
Formula | C18H26Cl2N4O3S |
Cas No. | 913844-45-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | PBS (pH 7.2): 10 mg/mL DMSO: 10 mg/mL Ethanol: 2 mg/mL DMF: 5 mg/mL |
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