PROTAC BET Degrader-12

• UNSPSC Description:

  PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and BRD4 in a DCAF11-dependent manner. PROTAC BET Degrader-12 inhibits cell viability of KBM7 with a DC50 of 305.2 nM. (Pink: ligand for target protein (+)-JQ-1 (HY-13030); Black: linker (HY-159077); Blue: ligand for E3 ligase (HY-159076))[1]

• Target Antigen:

  Epigenetic Reader Domain; PROTACs

• Type:

  Reference compound

• Related Pathways:

  Epigenetics;PROTAC

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/protac-bet-degrader-12.html

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  CC1=NN=C2[C@@H](N=C(C3=C(N12)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCCCCCNC(COC5=CC=C(C=C5)CNC(/C(C#N)=C/C6=CC=C7C=CC=CC7=C6)=O)=O)=O

• Molecular Weight:

  867.46

• References & Citations:

  [1]Tin G, et al., Discovery of a DCAF11-dependent cyanoacrylamide-containing covalent degrader of BET-proteins. Bioorg Med Chem Lett. 2024 Jul 15;107:129779.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  No Development Reported