VLX1570

DUB

-20

VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 ranging from 4.2 μM to 8.6 μM, and exhibits potent inhibition of USP14.

VLX1570 is a competitive inhibitor of proteasome DUB activity with IC50 ranging from 4.2 uM to 8.6 uM. It has potent inhibition for USP14. In vitor: VLX1570 was indeed found to inhibit USP14 in cells at a concentration of 1 uM. target: DUBs IC50: 4.2 uM to 8.6 uM In vitro: 1) VLX1570 inhibits proteasome deubiqu-itinase activity and induces accumulation of high molecularweight. polyubiquitinated proteins in cells. 2) Knock-down of USP14 in multiple myeloma cells induces loss of cell viability. 3) VLX1570 induces accumulation of polyubiquitin chains and elicits apoptosis of multiple myeloma cells. 4) VLX1570 induces apoptosis and cell death of MM cells In vivo: The reference for the injection is 5 mg/kg Note: The compound was dissolved in 50% PEG400/40%Tween-80/10% Kolliphor EL and then diluted with saline.