dBET1

SKU: orb1302813

Description

dBET1 is a cereblon-directed PROTAC that degrades BET proteins with an in vitro EC50 of 430 nM, leading to apoptosis. This molecular tool is widely used in oncology research to study BET protein function and has demonstrated activity in cellular and animal models of cancer.

Research Area

Epigenetics & Chromatin, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1799711-21-9
• MW: 785.27
• Purity: 98.02% (May vary between batches)
• Formula: C₃₈H₃₇ClN₈O₇S
• SMILES: CC=1C2=C(N3C([C@H](CC(NCCCCNC(COC4=C5C(C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=CC=C4)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C
• Target: Epigenetic Reader Domain,PROTACs
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (4.2 mM);DMSO:50 mg/mL (63.67 mM);H2O:Insoluble;Ethanol:5 mg/mL (6.37 mM)

Bioactivity

• Target IC50:
  BET:430 nM (EC50)
• In Vitro:
  dBET1 induced a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50 = 0.14 μM, compared to IC50 = 1.1 μM with JQ1) consistent with the reported, pronounced inhibitory effect of RNA silencing of BRD4 in this and other models of MLL-rearranged leukemia.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PROTACs, dBET1, dBET-1, dBET 1, BET, inhibit, Epigenetic Reader Domain, EpigeneticReaderDomain, Inhibitor

Compound Identifiers

PubChem CID

91799313