PROTAC Bcl2 degrader-1

PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN) -binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1[1] (Blue: CRBN ligand, Black: linker; Pink: Mcl-1/Bcl-2 inhibitor, Nap-1) .

Product Specifications

CAS Number

[2378801-85-3]

UNSPSC

12352005

Target

Bcl-2 Family; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bcl2-in-1.html

Purity

99.80

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(NCCOCCOCCNC1=CC=CC(C(N2C3CCC(NC3=O)=O)=O)=C1C2=O)CCCCC(NCCN4C(C5=C6C(C4=O)=CC=C(C6=CC=C5)SC7=CC=C(C=C7)Br)=O)=O

Molecular Formula

C45H45BrN6O10S

Molecular Weight

941.84

References & Citations

[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.