TAPI-2 | ADAM17 inhibitor | Probechem Biochemicals

Chemical Structure : TAPI-2

CAS No.: 187034-31-7

TAPI-2 (TNF Protease Inhibitor 2)

Catalog No.: PC-42086Not For Human Use, Lab Use Only.

TAPI-2 is a broad-spectrum inhibitor of TNF-α converting enzyme (TACE, ADAM17), ADAMs, and other MMPs, inhibits ADAM8, 10, 12, and TACE with Ki values of 10, 3, 100, and 0.12 uM, respectively.

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2 mg	$198	In stock
5 mg	$328	In stock
10 mg	$528	In stock
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Biological Activity

TAPI-2 is a broad-spectrum inhibitor of TNF-α converting enzyme (TACE, ADAM17), ADAMs, and other MMPs, inhibits ADAM8, 10, 12, and TACE with Ki values of 10, 3, 100, and 0.12 uM, respectively.

TAPI-2 inhibits PMA-induced shedding of cell surface proteins, such as TGF-α, β amyloid precursor protein, L-selectin, and IL-6 receptor α subunit in CHO cells with IC50 of 10 uM.

TAPI-2 reverses the malignant phenotype in a breast cancer cell line by preventing mobilization of the growth factors TGF-α and amphiregulin.

TAPI-2 binds to hmeprin with inhibition constants IC50 20±10 μM for hmeprin β subunit and 1.5±0.27 nM for hmeprin α subunit.

TAPI-2 dramatically decreases the protein levels of NICD and its downstream target HES-1 in both HCP-1 and HT29 cells.

TAPI-2 significantly decreases the CSC phenotype by -50% in treated CRC cell lines.

TAPI-2 is an ADAM17 inhibitor but not ADAM10 inhibitor.

Physicochemical Properties

M.Wt	415.5276
Formula	C19H37N5O5
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	DMSO: ≥ 22 mg/mL
Chemical Name/SMILES	L-Alaninamide, N-[2-[2-(hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-methyl-L-valyl-N-(2-aminoethyl)-

References

1. Moss ML, et al. Anal Biochem. 2007 Jul 15;366(2):144-8.

2. Parvathy S, et al. Biochem J. 1997 Oct 1;327 ( Pt 1):37-43.

3. Kenny PA, et al. J Clin Invest. 2007 Feb;117(2):337-45.

4. Fiorucci S, et al. Aliment Pharmacol Ther. 1998 Nov;12(11):1139-53.

TAPI-2 (TNF Protease Inhibitor 2)

Biological Activity

Physicochemical Properties

References

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