TGFβ1-IN-3

SKU: orb1982419

Description

TGFβ1-IN-3 is a diarylhydrazone-based small molecule inhibitor that suppresses fibroblast activation and proliferation. It serves as a research tool for studying fibrotic pathways and has shown potential in preclinical models of idiopathic pulmonary fibrosis (IPF).

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2883813-58-7
• MW: 442.51
• Purity: 99.73% (May vary between batches)
• Formula: C₂₃H₃₀N₄O₅
• SMILES: C(=N/NC(=O)C1=CC=C(OCCCCCCN2CCCCC2)C=C1)\C=3OC(N(=O)=O)=CC3
• Target: TGF-beta/Smad,Others
• Solubility: DMSO:45 mg/mL (101.69 mM)

Bioactivity

• In Vivo:
  TGFβ1-IN-3 (compound 44) administered orally at 30-60 mg/kg once daily for 22 days in C57BL/6 mice slows IPF progression and enhances lung function, potentially reversing pulmonary fibrosis in a treatment model.
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• In Vitro:
  TGFβ1-IN-3 (compound 44) inhibits NIH-3T3 cells with an IC50 of 0.57 μM. At 10 μM for 24 hours, it inhibits TGF-β1-induced abnormal activation of NIH-3T3 and A549 cells, as well as migration and epithelial-mesenchymal transition (EMT) of A549 cells. TGFβ1-IN-3 binds to STAT3, interacting with Ile659, while the hydrophilic piperidine forms intermolecular forces with Ser636, Arg609, and Pro639. The nitrofuran of TGFβ1-IN-3 interacts with Lys658.
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Storage & Handling

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

Compound Identifiers

PubChem CID

166177005