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SB525334
Name:
SB525334
Catlog NO.: CFC2126
CAS No.: 356559-20-1
Formula: C21H21N5
Spec/Purity: 99%
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Category: API

Molecular Structure
Memo:


SB525334 is a potent and selective inhibitor of TGF receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
IC50 value: 14.3 nM
Target: ALK5
in vitro: SB 525334 shows no inhibition in the enzymes ALK2, 3, and 6, with IC50 values > 10 M. SB 525334 blocks phosphorylation induced by TGF-1 and nuclear translocation of Smad2/3 in renal proximal tubule cells. SB 525334 also inhibits the increased mRNA expression levels of plasminogen activator inhibitor-1 (PAI-1) and procollagen 1(I) induced by TGF-1 in A498 renal epithelial carcinoma cells at 1 M) . SB 525334 (1 M) attenuates the heightened sensitivity to TGF-1 exhibited by pulmonary artery smooth muscle cells (PASMCs) from patients with familial forms of idiopathic pulmonary arterial hypertension (PAH) .
in vivo: SB 525334 (10 mg/kg/day) decreases the renal mRNA levels of PAI-1, procollagen 1(I), and procollagen 1(III) in a nephritis-induced renal fibrosis rat model. Furthermore, PAN-induced proteinuria is significantly inhibited by SB 525334 (10 mg/kg/day) [1]. SB 525334 may also be efficacious in mesenchymal tumors. SB 525334 (10 mg/kg/day) significantly decreases uterine mesenchymal tumor incidence, multiplicity, and size in Eker rats.



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