GSK-25

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].

Product Specifications

CAS Number

[874119-56-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Ribosomal S6 Kinase (RSK) ; ROCK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton; MAPK/ERK Pathway; Stem Cell/Wnt; TGF-beta/Smad

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/gsk-25.html

Concentration

10mM

Purity

99.68

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

ClC1=CC(C2=NC(C3=C(F)C=C(Cl)C=C3)C(C(NC4=C(F)C=C(NN=C5)C5=C4)=O)=C(C)N2)=CC=N1

Molecular Formula

C24H16Cl2F2N6O

Molecular Weight

513.33

Precautions

H302, H315, H319, H335

References & Citations

[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.