SB525334 (Synonyms: TGF-β RI Kinase Inhibitor VIII) |
Catalog No.GC14349 |
(TGF-beta1) receptor inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 356559-20-1
Sample solution is provided at 25 µL, 10mM.
SB525334 is a potent inhibitor of transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). It specifically inhibits ALK5 with IC50 value of 14.3nM, which shows 4-fold higher potency against ALK4 [1].
SB525334 has been demonstrated to reduce smad2/3 nuclear fluorescence induced by TGF-beta1 in human renal proximal tubule epithelial (RPTE) cells. Additionally, SB525334 inhibits TGF-beta1 mediated procollagen and PAI-1 expression in human renal carcinoma cells A498 [1].
SB525334 dose-dependently reduces Urinary protein, procollagen alpha1(I) mRNA and procollagen alpha1(III) mRNA when administered orally in acute puromycin aminonucleoside (PAN) rat model of renal disease [1].
Reference:
[1] Grygielko ET1, Martin WM, Tweed C, Thornton P, Harling J, Brooks DP, Laping NJ. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther. 2005 Jun;313(3):943-51.
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