IN-1130

SKU: orb1707181

Description

IN-1130 is a potent and selective ALK5 inhibitor, demonstrating IC50 values of 5.3 nM for ALK5-mediated Smad3 phosphorylation, 36 nM for casein phosphorylation, and 4.3 µM for p38α MAPK. This small molecule is a valuable research tool for investigating TGF-β signaling pathways in both cellular and animal models of fibrosis and cancer.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 868612-83-3
• MW: 420.47
• Purity: 99.79% (May vary between batches)
• Formula: C₂₅H₂₀N₆O
• SMILES: Cc1cccc(n1)-c1nc(Cc2cccc(c2)C(N)=O)[nH]c1-c1ccc2nccnc2c1
• Target: TGF-beta/Smad,ALK
• Solubility: DMSO:90 mg/mL (214.05 mM);10% DMSO+90% Saline:1 mg/mL (2.38 mM)

Bioactivity

• In Vivo:
  In unilateral ureteral obstruction rats, intraperitoneal administration of IN-1130 (10-20 mg/kg) decreases the extent of interstitial nephritis and fibrosis. dose-dependently reduces the levels of TGF-β1 mRNA and suppresses Smad2, α-SMA, myofibroblasts phosphorylation. In MMTV/c-Neu mice intraperitoneal administration of IN-1130 (40 mg/kg) blocks breast cancer lung metastasis.
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• In Vitro:
  IN-1130 (0.5 -1 μM) inhibits the phosphorylation and nuclear translocation of TGF-β-stimulated Smad2 in HepG2 and 4T1 cells. In MCF10A cells, IN-1130 (1 μM) restores the TGF-β-mediated decrease in E-cadherin protein expression, inhibits TGF-β-induced MMPs mRNA expression, and reduces the gelatinolytic activity of secreted MMPs.
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Storage & Handling

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

Alternative Names

IN 1130, IN1130, IN-1130, ALK5

Compound Identifiers

PubChem CID

11676119