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.
性状
Solid
IC50 & Target[1][2]
Mcl-1 0.78 μM (IC50) Bcl-2 0.54 μM (IC
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Wang Z, et al. Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands. J Med Chem. 2019 Aug 21.
溶解度数据
In Vitro: DMSO : 50 mg/mL (54.95 mM; Need ultrasonic)配制储备液