Microtubule destabilizing agent-3 is an analogue of B32B3 and functions as a microtubule destabilizer. By destabilizing microtubules and promoting mitotic arrest, it exerts its anti-myeloma phenotype, ultimately leading to cell death. Microtubule destabilizing agent-3 induces G2/M phase arrest and caspase-dependent apoptosis (apoptosis) and can be utilized in research on multiple myeloma.

Microtubule destabilizing agent-3 (VPR8) at a concentration of 500 nM for 24-48 hours induces significant cell death in the JJN3 cell line, with an IC50 value of approximately 190 nM, causes G2M phase arrest, and triggers apoptosis. At 500 nM for 1-24 hours, it upregulates signals related to the G2/M phase and autophagy while downregulating MYC signaling. When used at 0.25-20 μM for 24 hours, this agent does not reduce levels of H2AT120P, EZH2, or H3K27me3 in multiple myeloma cells. In CETSA experiments, Microtubule destabilizing agent-3 enhances the thermal stability of DCAF1.

Microtubule destabilizing agent-3 (VPR8), administered at 15 mg/kg via intraperitoneal injection for 5 consecutive days with a 2-day break, significantly delayed tumor progression and increased survival rates in xenograft mouse models of multiple myeloma and lymphoma.