A-385358

• CAT Number: I020440
• CAS Number: 406228-55-5
• Molecular Formula: C₃₂H₄₁N₅O₅S₂
• Molecular Weight: 639.83
• Purity: ≥95%
• Target: Bcl-2 Family

A-385358 (CAT: I020440) is a selective inhibitor of Bcl-XL, a member of the Bcl-2 family of proteins that regulate apoptosis. It exhibits a strong affinity for Bcl-XL with a Ki of 0.80 nM and moderate affinity for Bcl-2 with a Ki of 67 nM in fluorescence polarization assays. Treatment of IL-3-deprived FL5.12/Bcl-XL cells with A-385358 results in cell killing accompanied by increased caspase-3 activity, indicating its pro-apoptotic effect. A-385358 shows a higher potency in inducing cytochrome c release from mitochondria in FL5.12/Bcl-XL cells compared to FL5.12/Bcl-2 cells, further supporting its selective action on Bcl-XL.

Reference

[1]. Shoemaker AR, et al. A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo. Cancer Res. 2006 Sep 1;66(17):8731-9.