TAPI-2


CAS No. : 187034-31-7

187034-31-7
Price and Availability of CAS No. : 187034-31-7
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1mg $150 In-stock
5mg $600 In-stock
10mg $950 In-stock
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Cat. No. : HY-100211
M.Wt: 415.53
Formula: C19H37N5O5
Purity: >98 %
Storage: at -20℃ 3 years
Solubility: DMSO: ≥ 22 mg/mL
Introduction of 187034-31-7 :

TAPI-2 is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20±10 μM for MMP. IC50 & Target: IC50: 20±10 μM (MMP)[1] Ki: 1.5±0.27 nM (MMPs)[1] In Vitro: The hydroxamate-based metalloprotease inhibitor TAPI-2 bounds to hmeprin with inhibition constants IC50 20±10 μM for hmeprin β subunit and 1.5±0.27 nM for hmeprin α subunit. Generally, hmeprin α is inhibited more strongly than the β subunit[1]. Without affecting ADAM17 expression, TAPI-2 dramatically decreases the protein levels of NICD and its downstream target HES-1 in both HCP-1 and HT29 cells. Moreover, treating cells with TAPI-2 significantly decreases the CSC phenotype by -50% in both CRC cell lines. The dose-dependent effects of TAPI-2 on the sphere formation and protein levels of NICD and HES-1 confirm that the concentration used (20 μM) is within the effective dose range of TAPI-2 (5–40 μM)[2].

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