WX-02-16

WX-02-16 (5-50 μM; overnight) covalently modifies C126 of recombinant WT BAX, and the C126A mutation abolishes adduct formation even when the WX-02-16:BAX ratio reaches 50:1^[1].
WX-02-16 (50-500 nM; 45 min) inhibits tBID-induced, BAX-mediated cytochrome c release from purified mouse liver mitochondria in a dose-dependent manner and in a C126-dependent manner^[1].
WX-02-16 (2-20 μM; 45 min) inhibits tBID-triggered translocation of monomeric BAX to isolated mouse liver mitochondria in a dose-dependent manner^[1].
WX-02-16 (1-6 h) protects HCT116 Bak-/- cells from ABT-737 (HY-50907)/S63845 (HY-100741)-induced apoptosis in a BAX-dependent manner, whereas it has no protective effect on HCT116 Bax-/- cells^[1].
WX-02-16 (20 μM; 3 h) stereoselectively binds BAX in Ramos cells in protein-directed ABPP, binding to BAX C126 with a target engagement rate of >75%^[1].
WX-02-16 (20 μM; 2 h) binds BAX in HCT116 Bak-/- cells and is enriched as a top target in protein-directed ABPP^[1].
WX-02-16 (12-24 h) protects primary rat DRG neurons from ABT-737-induced apoptosis in a concentration-dependent manner^[1].
WX-02-16 blocks Cisplatin (HY-17394)-induced apoptosis in iBMK Bak-/- cells, but does not block apoptosis in iBMK Bax-/- cells^[1].