| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| S408793-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $55.90 |
TGFβRI/ALK5 Selective Inhibitors
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Storage Temp | Store at -80°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | Information SB525334 is a potent and selective inhibitor ofTGFβ receptor I (ALK5)withIC50of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. SB 525334 shows no inhibition in the enzymes ALK2, 3, and 6, with IC50 values > 10 μM. SB 525334 blocks phosphorylation induced by TGF-β1 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 α1(I) induced by TGF-β1 in A498 renal epithelial carcinoma cells at 1 μM). SB 525334 (1 μM) attenuates the heightened sensitivity to TGF-β1 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 α1(I), and procollagen α1(III) in a nephritis-induced renal fibrosis rat model. Furthermore, PAN-induced proteinuria is significantly inhibited by SB 525334 (10 mg/kg/day). 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. SB 525334 significantly reverses pulmonary arterial pressure and inhibits right ventricular hypertrophy in a rat model of PAH. This is revealed by a significant reduction in pulmonary arteriole muscularization induced by monocrotaline (used to induce PAH) after treatment with SB 525334 (3 or 30 mg/kg). In a Bleomycin-induced pulmonary fibrosis mice model, SB 525334 (10 mg/kg or 30 mg/kg) attenuates the histopathological alterations in the lung, and significantly decreased mRNA expression of Type I and III procollagen and fibronectin. SB 525334 also attenuates Smad2/3 nuclear translocation, myofibroblast proliferation, deposition of Type I collagen, and decreases CTGF-expressing cells. cell lines：GH3 cells Concentrations：1 μM Incubation Time：1 hour Powder Purity:≥99% |
| Canonical SMILES | CC1=NC(=CC=C1)C2=C([NH]C(=N2)C(C)(C)C)C3=CC=C4N=CC=NC4=C3 |
|---|---|
| Molecular Weight | 343.42 |
Enter Lot Number to search for COA:
| Solubility | Solubility (25°C) In vitro DMSO: 47 mg/mL (197.34 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
