TAPI-1

SKU: orb1689827

Description

TAPI-1 is a cell-permeable inhibitor of ADAM17/TACE that effectively blocks the ectodomain shedding of cytokine receptors and other transmembrane proteins. This small molecule is widely used in both in vitro and in vivo research to investigate inflammation, cancer, and signaling pathways dependent on regulated proteolysis.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 163847-77-6
• MW: 499.6
• Purity: ≥95%
• Formula: C₂₆H₃₇N₅O₅
• SMILES: CC(C)C[C@H](CC(=O)NO)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](C)C(=O)NCCN
• Target: MMP
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.61 mM);Ethanol:92 mg/mL (184.15 mM);DMSO:92 mg/mL (184.15 mM);H2O:55 mg/mL (110.09 mM)

Bioactivity

• In Vitro:
  TAPI-1 prevents unstimulated and PMA-induced release of the soluble forms of TNF-alpha, p60 TNFR, and IL-6R from the monocytic cell line, THP-1, and from human peripheral blood monocytes. TAPI also inhibits LPS-induced shedding of the p60 TNFR and TNF-alpha from monocytes. TAPI-1 inhibits TACE-dependent constitutive release of co-transfected APP(695). TAPI-1 attenuates Ang II-induced EGFR transactivation and cell proliferation in human HSC line LI90. TAPI-1 with the EGFR inhibitor AG1478 exhibits deactivated AREG/EGFR/ERK signaling pathway and reduces pro-inflammatory cytokines release in pSS salivary gland-derived epithelial cells.
• Cell Research:
  Five thousand cells are seeded into each well of 96-well plates and their viability is assessed by CellTiter-Glo Luminescent Cell Viability assay. Upon serum deprivation for 24 h, the cells are treated with Ang II for 60 h with and without pretreatment with each inhibitor and antagonist. The assay substrates are then added to each well on the plate and the samples are evaluated using a luminometer. (Only for Reference)

Storage & Handling

• Storage: store at low temperature,keep away from moisture | 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

Inhibitor, Matrix metalloproteinases, MMP, inhibit, cell surface proteins, ADAM17/TACE, TAPI, TAPI 1, TAPI1, TAPI-1, TAPI-1 Isomer

Compound Identifiers

PubChem CID

10458621