A PROTAC that drives Mcl-1 degradation
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PROTAC Mcl Degrader-1

Item No. 45150

Technical Information
Formal Name
N1-[2-[6-[(4-bromophenyl)thio]-1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl]ethyl]-N6-[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]hexyl]-hexanediamide
CAS Number
2163793-38-0
Synonyms
  • Proteolysis-targeting Chimera Mcl Degrader-1
Molecular Formula
C45H45BrN6O8S
Formula Weight
Purity
≥98%
A solid
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C(N1CCNC(CCCCC(NCCCCCCNC2=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/C45H45BrN6O8S/c46-27-15-17-28(18-16-27)61-35-21-19-32-39-29(35)9-7-10-30(39)42(57)51(43(32)58)26-25-49-37(54)14-4-3-13-36(53)48-24-6-2-1-5-23-47-33-12-8-11-31-40(33)45(60)52(44(31)59)34-20-22-38(55)50-41(34)56/h7-12,15-19,21,34,47H,1-6,13-14,20,22-26H2,(H,48,53)(H,49,54)(H,50,55,56)
InChi Key
BORXNUWYWZOREQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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    Product Description

    PROTAC Mcl degrader-1 is a proteolysis-targeting chimera (PROTAC) composed of a myeloid cell leukemia-1 (Mcl-1) inhibitor conjugated to the cereblon (CRBN) inhibitor pomalidomide (Item No. 19877) via an alkyl linker.1 It induces degradation of Mcl-1 in HeLa cells with a half-maximal degradation concentration (DC50) value of 0.76 µM. PROTAC Mcl degrader-1 induces selective degradation of Mcl-1 over Bcl-2, Bcl-xL, murine double minute 2 (MDM2), and tubulin in HeLa cells when used at a concentration of 10 µM. It inhibits the growth of H23 non-small cell lung cancer (NSCLC) cells in a concentration-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, Z., He, N., Guo, Z., et alProteolysis 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).