PROTAC Bcl-2 Degrader-1

PROTAC Bcl-2 degrader-1 is a proteolysis-targeting chimera (PROTAC) composed of a Bcl-2 inhibitor conjugated to the cereblon (CRBN) inhibitor pomalidomide (Cay19877) via a PEG linker. It induces the degradation of Bcl-2 in HeLa cells with a half-maximal degradation concentration (DC50) value of 3 µM. PROTAC Bcl-2 degrader-1 induces selective degradation of Bcl-2 over myeloid cell leukemia-1 (Mcl-1), Bcl-xL, murine double minute 2 (MDM2), and tubulin in HeLa cells when used at a concentration of 10 µM.. SMILES: O=C(N1CCNC(CCCCC(NCCOCCOCCNC2=C(C(N3C(CCC4=O)C(N4)=O)=O)C(C3=O)=CC=C2)=O)=O)C(C5=C6C=CC=C5C1=O)=CC=C6SC(C=C7)=CC=C7Br. InChi Code: InChI=1S/C45H45BrN6O10S/c46-27-11-13-28(14-12-27)63-35-17-15-32-39-29(35)5-3-6-30(39)42(57)51(43(32)58)22-19-48-36(53)9-1-2-10-37(54)49-21-24-62-26-25-61-23-20-47-33-8-4-7-31-40(33)45(60)52(44(31)59)34-16-18-38(55)50-41(34)56/h3-8,11-15,17,34,47H,1-2,9-10,16,18-26H2,(H,48,53)(H,49,54)(H,50,55,56). InChi Key: IUSLKFLLLNNOGR-UHFFFAOYSA-N