Biochem/physiol Actions

Cell permeable: no

Reversible: no

Primary TargetMMPs and TACE

Target IC₅₀: 8.09 µM and 3.61 µM blocking constitutive and muscarinic receptor-stimulated sAAPα release in HEK 293 cells expressing M3 muscarinic receptors, respectively

Product does not compete with ATP.

General description

A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α convertase; ADAM17). However, TAPI-1 is more stable in serum than TAPI-0. TAPI-1 Blocks the shedding of several cell surface proteins such as TNF-α, IL-6 receptor, and p60 and p80 TNF receptors. Inhibits constitutive (IC₅₀ = 8.09 µM) and muscarinic receptor-stimulated (IC₅₀ = 3.61 µM) sAPPa release in HEK-293 cells expressing muscarinic receptors. Also blocks the TACE-dependent constitutive release of co-transfected APP(695) (IC₅₀ = 920 nM).

A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α converting enzyme/ADAM17). TAPI-1 also blocks the shedding of several cell surface proteins such as IL-6 receptor, p60 TNF receptor, and p80 TNF receptor. Blocks constitutive (IC₅₀ = 8.09 µM) and muscarinic receptor-stimulated (IC₅₀ = 3.61 µM) sAAPα release in HEK 293 cells expressing M3 muscarinic receptors. A 10 mM (500 µg/100 µl) solution of TAPI-1 (Cat. No. 579050) in DMSO is also available.

Legal Information

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

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

Other Notes

Slack, B.E., et al. 2001. Biochem. J.357, 787.Vincent, B., et al. 2001. J. Biol. Chem.276, 37743.Hooper, N.M., et al. 1997. Biochem. J.321, 265.Crowe, P.D., et al. 1995. J. Exp. Med.181, 1205.Mullberg, J., et al. 1995. J. Immunol.155, 5198.Mohler, K.M., et al. 1994. Nature370, 218.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Standard Handling (A)