PROTAC Bcl2 degrader-1

• CAS Number:

  2378801-85-3

• UNSPSC Description:

  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).

• Target Antigen:

  Bcl-2 Family; PROTACs

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;PROTAC

• 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 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, stored under nitrogen)

• Clinical Information:

  No Development Reported