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).
Biochem/physiol Actions
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
