LY3200882

SKU: orb1302068

Description

LY3200882 is a potent and selective TGFβRI kinase inhibitor. It is a valuable research tool for studying TGF-β signaling in cancer biology and fibrosis, with demonstrated utility in both cellular assays and in vivo animal models.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1898283-02-7
• MW: 435.52
• Purity: 99.63% (May vary between batches)
• Formula: C₂₄H₂₉N₅O₃
• SMILES: CC(C)(O)c1cc(Nc2cc(Oc3cn(nc3C3CCOCC3)C3CC3)ccn2)ccn1
• Target: TGF-beta/Smad
• Solubility: DMSO:4.36 mg/mL (10.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.3 mM)

Bioactivity

• Target IC50:
  TGFβRI:38.2 nM (IC50)
• In Vivo:
  LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose-dependent fashion. LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer) .
• In Vitro:
  LY3200882 effectively inhibits TGFβ-mediated SMAD phosphorylation in tumor and immune cells in vitro, demonstrates anti-metastatic activity in migration assays, and rescues TGFβ1 or T regulatory cell-suppressed naive T cell activity, restoring proliferation in immune suppression assays .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, immune, LY3200882, LY-3200882, LY 3200882, Inhibitor, ALK5, ATP-competitive, Anti-cancer, anti-metastatic, serine-threonine, phosphorylation, TGFb, TGF-b/Smad, TGFbeta/Smad, TGF-beta, TGFbeta, TGF-β Receptor, TGF-β/Smad, TGFβ, SMAD, Smad, TGF-βRI (ALK5), TGFβRI, Transforming growth factor beta receptors

Compound Identifiers

PubChem CID

121249291