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GSK-25

CAS No. : 874119-56-9

MCE 国际站：GSK-25

产品活性：GSK-25 是一种有效的、选择性的，具有口服活性的 ROCK1 抑制剂 (IC₅₀=7 nM)。GSK-25 对 31 种激酶以及 RSK1 和 p70S6K 保持良好的选择性 (RSK1: IC₅₀=398 nM, p70S6K: IC₅₀=1 µM)。GSK-25 可抑制 P450 (CYP2C9、CYP2D6、CYP3A4的IC₅₀ 分别为2.5、5.2、2.5 µM)。

研究领域：Cell Cycle/DNA Damage | Stem Cell/Wnt | Cytoskeleton | TGF-beta/Smad | MAPK/ERK Pathway

作用靶点：ROCK | Ribosomal S6 Kinase (RSK)

In Vivo: GSK-25 (Rat aorta IC₅₀=256 nM) is profiled in a spontaneously hypertensive rat (SHR) model of hypertension. At 30 mg/kg (p.o.), GSK-25 induces a 25 mmHg (t=3 hours) drop in blood pressure.
GSK-25 has promising oral bioavailability (49% in male Sprague-Dawley rats and 19% in monkey), good half-life (1.8 hours in rat and 2.2 hours in monkey).

相关产品：Covalent Screening Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | Anti-Aging Compound Library | Covalent Screening Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Anti-Cardiovascular Disease Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Glutamine Metabolism Compound Library | Y-27632 dihydrochloride | Chroman 1 | Fasudil Hydrochloride | PF-4708671 | Narciclasine | Ripasudil | Carnosol | GSK429286A | Pluripotin | Y-33075 | LJH685 | CMPD101 | H-1152 dihydrochloride | Sodium Salicylate | LJI308 | Quercitrin | Hydroxyfasudil | SL 0101-1 | BDP5290 | CKI⁻⁷ free base | AT7867 dihydrochloride | SR-3677 | SB⁻⁷72077B dihydrochloride | BRD7389 | Eudesmin | Pentanoic acid

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