PBRM1-BD2-IN-2

SKU: orb1689801

Description

PBRM1-BD2-IN-2 is a selective, cell-active small molecule inhibitor targeting the second bromodomain (BD2) of PBRM1, with a Kd of 9.3 µM and an IC50 of 1.0 µM. It is a valuable chemical probe for investigating the role of PBRM1 in oncology research, supporting both in vitro and in vivo studies of chromatin remodeling in cancer contexts.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2819989-57-4
• MW: 311.14
• Purity: >99.99% (May vary between batches)
• Formula: C₁₄H₉Cl₂FN₂O
• SMILES: O=C1C=2C(NC(N1)C3=C(Cl)C=CC=C3F)=CC=CC2Cl
• Target: Epigenetic Reader Domain
• Solubility: DMSO:45 mg/mL (144.63 mM)

Bioactivity

• In Vitro:
  PBRM1-BD2-IN-2 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibits the growth of a PBRM1-dependent prostate cancer cell line. It exhibits binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B, and SMARCA4 with Kd values of 9.3 μM, 10.1 μM, 18.4 μM, and 69 μM, respectively, and inhibits PBRM1-BD2 with an IC50 of 1.0 μM.
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Storage & Handling

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

Alternative Names

PBRM1BD2IN2, PBRM1-BD2-IN-2, EpigeneticReaderDomain, Epigenetic Reader Domain

Compound Identifiers

PubChem CID

164880750