BV6 is a bivalent Smac mimetic and an antagonist of the inhibitor of apoptosis (IAP) proteins that binds to IAP1 and XIAP (K
ds = 0.46 and 1.3 nM, respectively).
1 It induces autoubiquitination and proteasomal degradation of IAP1 and XIAP in MDA-MB-231 cells when used at a concentration of 5 μM. BV6 (4 μM) induces NF-κB activation and TNF-dependent apoptosis in A2058 and MDA-MB-231 cells. It enhances radiosensitization and increases apoptosis in HCC193 and H460 non-small cell lung cancer (NSCLC) cell lines.
2 BV6 (1 μM) induces cell death in a panel of 40 primary, patient-derived B cell precursor acute lymphoblastic leukemia (BCP-ALL) samples in a TNF-dependent manner.
3 In vivo, BV6 (10 mg/kg) increases survival and the time to relapse in a high-risk BCP-ALL patient-derived xenograft (PDX) mouse model.