PROTAC Mcl1 degrader-1

PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera ( PROTAC ) based on Cereblon ligand, is a potently and selectively Mcl-1 ( Bcl-2 family member) inhibitor with an IC 50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC 50 of 0.54 μM In Vitro PROTAC Mcl1 degrader-1 (compound C3) induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand Pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. ? PROTAC Mcl1 degrader-1 (0-10 μM; 0-24 h) induces selective depletion of Mcl-1 or Bcl-2 protein in HeLa cells in a time- and concentration-dependent manner. ? PROTAC Mcl1 degrader-1 (0-2 μM; 24 h) shows cytotoxicity against H23 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HeLa cells and H23 cells Concentration: 0.3, 1.0, 3.0 and 10 μM Incubation Time: 0-24 h Result: Induced time- and concentration-dependent selective depletion of Mcl-1 or Bcl-2 protein in HeLa cells. Induced Mcl-1 depletion and PARP cleavage in H23 cells (0-10 μM; 12 h). Form:Solid IC50& Target:Mcl-1 0.78 μM (IC 50 ) Bcl-2 0.54 μM (IC 50 )

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