GW788388 452342-67-5

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Molecular Weight:

425.48 GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.

Biological Activity

GW788388 shows anti-TGF-β activity with IC50 of 93 nM in cellular assay. GW788388 shows some inhibitory to activin type II receptor (ActRII) but
no inhibitory to bone morphogenic protein (BMP) type II receptor.
GW788388 shows no toxicity in Namru murine mammary gland (NMuMG),
MDA-MB-231, renal cell carcinoma (RCC)4, and U2OS cells at 4 nM to 15
μM. GW788388 blocks TGF-β-induced Smad activation and target gene
expression, while decreasing epithelial-mesenchymal transitions and
fibrogenesis. GW788388 inhibits ALK5, ALK4, ALK7 and TGF-β-mediated
growth arrest.


GW788388 exhibits an adequate pharmacokinetic profile in rats (plasma
clearance less than 40 mL/min/kg and half-life more than 2 hours).
GW788388 significantly reduces the expression of collagen IA1 mRNA by
80% in a model of puromycin aminonucleoside-induced renal fibrosis at 10
mg/kg. GW788388 attenuates TGF-β signalling and
effectively reduces hallmarks of fibrogenesis in mice suffering from
late-stage diabetic nephropathy at 2 mg/kg.


Treatment
with GW788388 significantly attenuates systolic dysfunction in the
myocardial infarction (MI) animals, together with the attenuation of the
activated (phosphorylated) Smad2, α-smooth muscle actin, and collagen I
in the noninfarct zone of MI rats. Cardiomyocyte hypertrophy in MI
hearts is also attenuated by GW788388 inhibition. GW788388 reduces the fibrotic response in bleomycin-injected animals at 2 mg/kg.

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Product Categories : TGF-beta/Smad