TAPI-1

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).

Cell permeable: no

Primary Target
MMPs and TACE

Product does not compete with ATP.

Reversible: no

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

Packaged under inert gas

A 10 mM (500 µg/100 µl) solution of TAPI-1 (Cat. No. 579051) in DMSO.

Following initial thaw, aliquot and freeze (-20°C).

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

Toxicity: Irritant (B)