An inhibitor of TACE that inhibits the cleavage of TNF-α

TAPI-1 – 5 mg

Brand:
Cayman
CAS:
171235-71-5
Storage:
-20
UN-No:
Non-Hazardous - /

TNF-α converting enzyme (TACE, also known as ADAM17) is a zinc metalloprotease that cleaves the membrane-bound precursor of TNF-α to give the mature soluble form of TNF-α.{24091,24093} It also mediates the proteolytic release of several other cell-surface proteins, including TNF-α receptors (TNFRs). TAPI-1, known in the earlier literature as just TAPI, is an inhibitor of TACE that inhibits the cleavage of TNF-α, TNFRI (p60), and TNFRII (p80) with IC50 values ranging from 5-100 µM.{24091,29961,24092} It also blocks the shedding of other TACE-dependent proteins, including IL-6R and Klotho, and may inhibit metalloproteases other than TACE.{24093,15600,29962} TAPI-1 differs from TAPI-0 (Item No. 14694), structurally, by the presence of an aminoethyl addition at the alanyl group, and is generally more stable in tissue culture and in vivo.  

 

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Description

An inhibitor of TACE that inhibits the cleavage of TNF-α, TNFRI (p60), and TNFRII (p80) with IC50 values ranging from 5-100 µM

Formal name: N-[2-[2-(hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-(2-naphthalenyl)-L-alanyl-N-(2-aminoethyl)- (9CI)L-alaninamide

Synonyms:  TAPI

Molecular weight: 499.6

CAS: 171235-71-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Immunology & Inflammation

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