(4-Benzylpiperazino)acetic acid-(3-allyl-2-hydroxybenzylidene)hydrazide
PAC-1 Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable allylsalicylidine hydrazone compound that activates procaspase-3 (EC50 = 220 nM) by overcoming the safety-catch-mediated suppression of caspase autoactivation. Substitution of any of the three aspartate residues in the enzyme′s safety-catch region greatly reduces the in vitro activation efficiency (EC50 = 2.77 µM, 113 µM, and 131 µM for mutant procaspase-3 with DAD, DDA, and ADD sequence, respectively; EC50 = 4.5 µM for wild-type procaspase-7 with DTD sequence) and the potency of apoptosis induction by PAC-1 in various cells strongly correlates with procaspase-3 cellular expression levels. Shown to induce tumor retardation and regression in several murine xenograft models in a dose-dependent manner in vivo. Purity: ≥95% by HPLC. Ref.: Putt, K.S., et al. 2006. Nat. Chem. Biol. 2, 543. |
