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KI2216GW7883885 mg$144
GW78838825 mg$432
GW788388100 mg$1202

Chemical Characteristic

Product NameGW788388
CAS No.452342-67-5
Molecular Weight 425.48242
FormulaC25H23N5O2
Chemical Name4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide
SmilesC(=O)(c1ccc(cc1)c1cc(ccn1)c1c(n[nH]c1)c1ccccn1)NC1CCOCC1
Chemical Structure

Biological activities

GW788388 is a potent and selective TGF-β type I receptor inhibitor. GW788388 inhibits both the TGF-β type I and type II receptor kinase activities, but has no effect on the BMP type II receptor kinase activity in vitro.[1] GW788388 also inhibits autophosphorylation of ALK5, TbRII, and ActRII.[2] The IC50 of GW788388 against GST-ALK5 is 18 nM.[2] GW788388 inhibits TGF-β-induced Smad2 phosphorylation in a dose-dependent manner in NMuMG, MDA-231-MB,and renal cell carcinoma.[2] GW788388 blocks the target gene expression and decreases epithelial??esenchymal transitions and fibrogenesis.[2] In vivo, in the mouse of diabetic nephropathy model, GW788388 significantly reduces renal fibrosis and decreases the mRNA levels of key mediators of extracellular matrix deposition in kidneys.[2] In a mouse allograft model, oral administration of BMS-554417??00 mg/kg once daily??hows significant antitumor efficacy in mice.[2] In addition, GW788388 reduces TGF-β activity and leads to the attenuation of systolic dysfunction and left ventricular remodeling in a rat model of myocardial infarction(MI).[3]

Protocols

In vivo: GW788388 is dissolved in DMSO.[4]

References

[1] 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(7): 2210-2221.
[2] 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.
[3] 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-H1425.
[4] Lagares D, et al. Endothelin 1 contributes to the effect of transforming growth factor beta1 on wound repair and skin fibrosis. Arthritis Rheum. 2010, 62(3): 878-889.

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