GSK180736A

GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.

Product Specifications

CAS Number

[817194-38-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

G Protein-coupled Receptor Kinase (GRK) ; ROCK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton; GPCR/G Protein; Stem Cell/Wnt; TGF-beta/Smad

Applications

COVID-19-anti-virus

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/GSK180736A.html

Purity

98.81

Solubility

DMSO : ≥ 30 mg/mL

Smiles

CC(N1)=C(C(NC2=CC=C(NN=C3)C3=C2)=O)C(C4=CC=C(F)C=C4)NC1=O

Molecular Formula

C19H16FN5O2

Molecular Weight

365.36

Precautions

H302, H315, H319, H335

References & Citations

[1]Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59 (8) :3793-807.