579052

TAPI-2

TAPI-2, CAS 187034-31-7, is a hydroxamate-based inhibitor of MMPs and TACE. Inhibits the activation-induced shedding of L-selectin from neutrophils, eosinophils, and lymphocytes.

• Synonym(s): TAPI-2, N-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L- t-butyl-alanyl-L-alanine, 2-aminoethyl Amide, TNF-α Protease Inhibitor-2, N-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-t-butyl-alanyl-L-alanine, 2-aminoethyl Amide, TNF-α Protease Inhibitor-2
• Empirical Formula (Hill Notation): C₁₉H₃₇N₅O₅
• CAS Number: 187034-31-7
• Molecular Weight: 415.53
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: ethanol: 5 mg/mL; water: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

A hydroxamate-based inhibitor of MMPs and TACE. Inhibits the activation-induced shedding of L-selectin from neutrophils, eosinophils, and lymphocytes, as well as phenylarsine oxide (PAO)-induced shedding in neutrophils. Also acts as a weak inhibitor of angiotensin converting enzyme (IC₅₀ = 18 µM). Also available as a 10 mM solution in H₂O (Cat. No. 509612).

A hydroxamate-based inhibitor of matrix metalloproteinases and TACE (TNF-α convertase; ADAM17). Inhibits the activation-dependent shedding of L-selectin from neutrophils, eosinophils, and lymphocytes as well as phenylarsine oxide (PAO)-induced shedding in neutrophils. Also blocks the shedding of several cell surface proteins such as pro-TGF-α, IL-6 receptor α-subunit, and β-amyloid precursor protein. Reported to inhibit TNF-α release and impart protection against aspirin-induced gastric mucosal injury. Acts as a weak inhibitor of angiotensin converting enzyme (IC₅₀ = 18 µM).

Biochem/physiol Actions

Cell permeable: no

Primary Target
MMPs

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 18 µM against angiotensin converting enzyme

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Bennett, T.A., et al. 2000. J. Immunol.164, 4120.
Fiorucci, S., et al. 1998. Aliment. Pharmacol. Ther.12, 1139.
Hooper, N.M., et al. 1997. Biochem. J.321, 265.
Parvathy, S., et al. 1997. Biochem. J. 327, 37.
Arribas, J., et al. 1996. J. Biol. Chem.271, 11376.

Legal Information

Manufactured exclusively by Peptides International, Louisville, Kentucky, USA.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable