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TNF Protease Inhibitor 2

Catalog No. TQ0129 CAS 187034-31-7

Synonyms: TAPI-2

TAPI-2 is a broad-spectrum inhibitor of MMP (IC50: 20 μM), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM).

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TNF Protease Inhibitor 2, CAS 187034-31-7

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Purity 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

TAPI-2 is a broad-spectrum inhibitor of MMP (IC50: 20 μM), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM).

In vitro

TAPI-2 bounds to h-meprin with IC50 20 μM for h-meprin β subunit and 1.5 nM for h-meprin α subunit. Generally, h-meprin 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].

Synonyms	TAPI-2
Molecular Weight	415.53
Formula	C19H37N5O5
CAS No.	187034-31-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 20 mg/mL (48.13 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature

1. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. 2. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.