| Description |
A cell-permeable pyrazolone compound that triggers Bax conformational changes by targeting Bax N-terminal face "BH3 trigger site" formed by the confluence of α-helices 1 &2 in a reversible manner (IC 50 = 4.41 µM against 50 nM BIM BH3-derived FITC-BIM SAHB peptide for Bax binding), leading to dose-dependent Bax oligomerization induction, Bax mitochondria translocation, and eventual Bax-dependent apoptotic cell death (33%, 90% and 94% survival rate in Bak -/- , Bak -/- Bax -/- , and Bax -/- MEF cultures, respectively; 10 µM for 24 h)
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