GW788388

GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.

Product Specifications

CAS Number

[452342-67-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H320, H335

Target

TGF-β Receptor

Type

Reference compound

Related Pathways

TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GW788388.html

Purity

99.92

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C=C1)C2=NC=CC(C3=CNN=C3C4=NC=CC=C4)=C2)NC5CCOCC5

Molecular Formula

C25H23N5O2

Molecular Weight

425.48

Precautions

H302, H315, H320, H335

References & Citations

[1]Petersen M, et al. Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int, 2008, 73 (6), 705-715.|[2]Tan SM, et al. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am J Physiol Heart Circ Physiol, 2010, 298 (5), H1415-1425.|[3]Gellibert F, et al. Discovery of 4-{4-[3- (pyridin-2-yl) -1H-pyrazol-4-yl]pyridin-2-yl}-N- (tetrahydro-2H- pyran-4-yl) benzamide (GW788388) : a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. J Med Chem. 2006, 49