Catalog No.: PC-49507Not For Human Use, Lab Use Only.
MS67 is a highly effective, selective WDR5 degrader (PROTAC), contains the E3 ligase ligand VHL-1 and WDR5 binding moiety, shows binding affinities to VCB (Kd=140 nM) and WDR5 (Kd=63 nM), potently and selectively degrades WDR5 in MLL-r AML and PDAC cells.
MS67 is a highly effective, selective WDR5 degrader (PROTAC), contains the E3 ligase ligand VHL-1 and WDR5 binding moiety, shows binding affinities to VCB (Kd=140 nM) and WDR5 (Kd=63 nM), potently and selectively degrades WDR5 in MLL-r AML and PDAC cells.
MS67 potently and selectively degrades WDR5 in MV4;11 cells at a concentration as low as 1 nM with DC50 of 3.7 nM (Dmax=94%), and DC50 of 45 nM in MIA PaCa-2 cells.
MS67 is effective in suppressing transcription of WDR5-regulated genes and H3K4me2 on chromatin.
MS67 exhibits significant inhibition of in vitro growth in a panel of MLL-r AML lines with IC50 of 15 and 38 nM for MV4;11 and EOL-1 cells, respectively.
MS67 (75-150 mg/kg, BID, i.p.) suppresses tumor growth in MV4;11 MLL-r AML xenograft mouse model, inhibits the growth of primary AML cells and improves survival in a PDX model.
