A PROTAC that drives Bcl-2 degradation
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PROTAC Bcl-2 Degrader-1

Item No. 45385

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-[2-[6-[(4-bromophenyl)thio]-1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl]ethyl]-N6-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]-hexanediamide
CAS Number
2378801-85-3
Synonyms
  • PROTAC BCL2 Degrader-1
  • Proteolysis-targeting Chimera Bcl-2 Degrader-1
  • Proteolysis-targeting Chimera BCL2 Degrader-1
Molecular Formula
C45H45BrN6O10S
Formula Weight
941.9
Purity
≥98%
Formulation (Request formulation change)
A solid
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    PROTAC Bcl-2 degrader-1 is a proteolysis-targeting chimera (PROTAC) composed of a Bcl-2 inhibitor conjugated to the cereblon (CRBN) inhibitor pomalidomide (Item No. 19877) via a PEG linker.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, Z., He, N., Guo, Z., et al. Proteolysis targeting chimeras for the selective degradation of Mcl-1/Bcl-2 derived from nonselective target binding ligands. J. Med. Chem. 62(17), 8152-8163 (2019).