BRD4/CK2-IN-1

SKU: orb1686049

Description

BRD4/CK2-IN-1 is a dual-target inhibitor of BRD4 (IC50=180 nM) and CK2 (IC50=230 nM). It demonstrates potent anti-proliferative effects in triple-negative breast cancer cell lines like MDA-MB-231 and MDA-MB-468 by inducing apoptosis and autophagy, making it a valuable tool for oncology research.

Research Area

Cell Biology, Epigenetics & Chromatin, Metabolism Research, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2756851-99-5
• MW: 564.03
• Purity: 99.02% (May vary between batches)
• Formula: C₂₉H₃₀ClN₅O₅
• SMILES: O=C1N=C(NC=2C=C(OC)C=C(OC)C12)C=3C=CC(OCC(=O)NC4=CC=C(C(Cl)=C4)N5CCN(C)CC5)=CC3
• Target: Epigenetic Reader Domain,Autophagy,Casein Kinase,Apoptosis
• Solubility: DMSO:16 mg/mL (28.37 mM)

Bioactivity

• Target IC50:
  CK2:230 nM|BRD4:180 nM
• In Vivo:
  In MDA-MB-468 and MDA-MB-231 xenograft tumor models, BRD4/CK2-IN-1 (25 mg/kg and 50 mg/kg) was administered intravenously and orally to inhibit tumor growth in a dose-dependent manner.
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• In Vitro:
  BRD4/CK2-IN-1 showed significant inhibitory activity against BRD4 (IC50 = 180 nM). BRD4/ CK2-in-1 showed significant inhibitory activity against CK2 (IC50 = 230 nM). BRD4/ CK2-in-1 induces TNBC cell death by targeting BRD4 and CK2. BRD4/ CK2-in-1 can bind to BRD4 and CK2 IN cells and inhibit BRD4 and CK2-regulated proliferation pathways, but has no significant effect on the protein levels of BRD4 and CK2.
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Storage & Handling

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

Compound Identifiers

PubChem CID

162641712