TMI-1

SKU: orb1699120

Description

TMI-1 (WAY-171318) is a potent, orally bioavailable dual inhibitor of ADAM17/TACE and matrix metalloproteinases (MMPs). This small molecule has been shown to induce apoptotic cell death in breast cancer models, supporting its use in oncology research for studying tumor biology and therapeutic targets in both in vitro and in vivo settings.

Research Area

Cell Biology, Immunology & Inflammation, Protein Biochemistry

Key Properties

• CAS Number: 287403-39-8
• MW: 398.5
• Purity: 98.79% (May vary between batches)
• Formula: C₁₇H₂₂N₂O₅S₂
• SMILES: CC#CCOc1ccc(cc1)S(=O)(=O)N1CCSC(C)(C)[C@@H]1C(=O)NO
• Target: MMP,TNF,Apoptosis,Caspase,ADAM,Interleukin
• Solubility: DMSO:35.9 mg/mL (90.09 mM)

Bioactivity

• Target IC50:
  MMP14:26 nM|TNF-α secretion (THP-1 cells):200 nM|ADAM17/TACE:0.079 nM(ki)|TNF-α secretion (Raw cells):40 nM|ADAM12:1.8 nM(ki)|ADAM17/TACE:8.4 nM (IC50)|MMP7:26 nM|MMP2:4.7 nM|ADAM8:21 nM(ki)|MMP1:6.6 nM|ADAMTS-4:100 nM|ADAM10:16 nM(ki)|MMP13:3 nM|MMP9:12 nM
  Read more...
• In Vivo:
  TMI 1 inhibits LPS-induced TNF-α production in mice (ED50 = 5 mg/kg) and reduces disease severity in mouse models of collagen-induced arthritis. It also decreases cell viability of (ED50s = 1.3-8.1 μM), and induces caspase-3/7 activity in, a variety of cancer cell lines and induces tumor apoptosis and reduces tumor growth in an MMTV-ErbB2/neu mouse model of breast cancer when administered at a dose of 100 mg/kg.
  Read more...
• In Vitro:
  TMI 1 inhibits LPS-induced TNF-α secretion in Raw and THP-1 cells (IC50s = 40 and 200 nM, respectively), as well as in isolated human monocytes and whole blood (IC50s = 190 and 300 nM, respectively). It inhibits the production of TNF-α ex vivo in synovium isolated from the inflamed joints of patients with rheumatoid arthritis with IC50 values of less than 100 nM without inhibiting TNF-α expression in vitro.
  Read more...

Storage & Handling

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

Alternative Names

ADAM17, apoptosis, TMI 1, TMI1, TMI-1, WAY171318, WAY-171318, WAY 171318

Compound Identifiers

PubChem CID

5288615