SB 525334

SKU: orb1225210

Description

SB 525334 is a potent and selective inhibitor of TGF-β1 receptor (ALK5) inhibitor with IC50 of 14,5 nM, 4-fold less potent against ALK4 and inactive for ALK2, ALK3, and ALK6 (IC50>10 uM); blocks TGFβ1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibits TGFβ1-induced increases in PAI-1 and procollagen α1 mRNA expression in A498 renal epithelial carcinoma cells at 1 uM; significantly inhibits PAN-induced proteinuria in rat model of nephritis-induced renal fibrosis.

Key Properties

• CAS Number: 356559-20-1
• MW: 343.4249
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₁N₅
• SMILES: CC1=CC=CC(C2=C(C3=CC=C4N=CC=NC4=C3)N=C(C(C)(C)C)N2)=N1
• Target: TGFBR
• Solubility: DMSO: ≥ 46 mg/mL

Bioactivity

• In Vivo:
  SB525334 (3-30 mg/kg; p.o. ; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH). Animal model: Adult male Sprague-Dawley rats (MCT rat model of pulmonary hypertension). Dosage: 3, 30 mg/kg. Administration: Oral administration; daily from days 17 to 35. Result: Reduced the proportion of fully muscularized vessels to 28% at 3 mg/kg and returned fully muscularized vessel distribution beyond that seen at day 17 and approaching the phenotype observed in saline-exposed controls at 30 mg/kg.
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• In Vitro:
  SB525334 (1 μM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-β1, assesses after 6 days) inhibits TGF-β1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC50 of 295 nM. Cell Proliferation Assay Cell line: PASMC cells. Concentration: 1 μM. Incubation time: Pre-incubated for 15 minutes (before stimulating with 0.625 ng/ml of TGF-β1), assessed after 6 days Result: Inhibited TGF-β1-mediated proliferation of familial iPAH PASMCs at an IC50 of 295 nM.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB-525334 | SB525334

Quick Database Links

Gene Symbol

TGFBR