874119-56-9

874119-56-9 structure

Name: 4-(4-chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-1-(6-fluoro-1H-indazol-5-yl)-6-methyl-4H-pyrimidine-5-carboxamide
Chemical Name: 4-(4-chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-1-(6-fluoro-1H-indazol-5-yl)-6-methyl-4H-pyrimidine-5-carboxamide
CAS Number: 874119-56-9
Molecular Formula: C₂₄H₁₆Cl₂F₂N₆O
Molecular Weight: 513.326
Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
Create Date: 2016-11-16 01:55:20
Modify Date: 2024-01-05 20:11:19
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively)[1].

Name	4-(4-chloro-2-fluorophenyl)-2-(2-chloropyridin-4-yl)-1-(6-fluoro-1H-indazol-5-yl)-6-methyl-4H-pyrimidine-5-carboxamide
Synonyms	4-(4-Chloro-2-fluorophenyl)-2-(2-chloro-4-pyridinyl)-N-(6-fluoro-1H-indazol-5-yl)-6-methyl-1,4-dihydro-5-pyrimidinecarboxamide 5-Pyrimidinecarboxamide, 4-(4-chloro-2-fluorophenyl)-2-(2-chloro-4-pyridinyl)-N-(6-fluoro-1H-indazol-5-yl)-1,4-dihydro-6-methyl-

Description	GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively)[1].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK Signaling Pathways >> MAPK/ERK Pathway >> Ribosomal S6 Kinase (RSK) Signaling Pathways >> Stem Cell/Wnt >> ROCK Signaling Pathways >> TGF-beta/Smad >> ROCK
Target	ROCK1:7 nM (IC50) RSK1:398 nM (IC50) p70S6K:1000 nM (IC50)
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[1]. 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)[1].
References	[1]. Sehon CA, et al. Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases. J Med Chem. 2008 Nov 13;51(21):6631-4.