BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis[1].
Biological Activity
BTSA1 is a BAX activator that binds to its N-terminal activation site with high affinity and specificity, induces a conformational change in BAX, and causes BAC-mediated apoptosis. It efficiently promotes apoptosis in leukemia cell lines and patient samples without affecting healthy cells.
in vivo
BTSA1 effectively inhibits human acute myeloid leukemia xenografts and enhances host survival without toxic side effects. In mice, it was well tolerated.
target
Target
Value
Bax ()
IC 50
Bax: 250 nM (IC50); Bax: 144 nM (EC50)
References
[1] Reyna DE, et al. Direct Activation of BAX by BTSA1 Overcomes Apoptosis Resistance in Acute Myeloid Leukemia. Cancer Cell. 2017 Oct 9;32(4):490-505.e10. DOI:10.1016/j.ccell.2017.09.001
