TRIM24/BRPF1-IN-2

SKU: orb1983078

Description

TRIM24/BRPF1-IN-2 is a potent and selective dual inhibitor of the epigenetic readers TRIM24 and BRPF1. It demonstrates dose-dependent anticancer activity in prostate cancer models by suppressing cell proliferation, target gene expression, and colony formation in vitro. This compound is a valuable chemical probe for researching bromodomain biology and oncology in cellular assays.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 3033288-68-2
• MW: 386.47
• Purity: 99.13% (May vary between batches)
• Formula: C₂₀H₂₂N₂O₄S
• SMILES: O=C(N1C2=CC=C(C=C2CC1)NS(=O)(=O)C3=CC(=CC=C3OC)C4CC4)C
• Target: Epigenetic Reader Domain

Bioactivity

• Target IC50:
  BRPF1:1.16 μM|C4-2B cells:0.78 μM|22Rv1 cells:0.82 μM|LNCaP cells:1.07 μM
• In Vivo:
  TRIM24/BRPF1-IN-2 administered once daily by intraperitoneal injection for 21 consecutive days at a dose of 50 mg/kg significantly inhibited tumor growth (TGI = 53%) and no significant toxicity was observed.
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• In Vitro:
  TRIM24/BRPF1-IN-2 significantly inhibited the growth of prostate cell lines (C4-2B, LNCaP, and 22Rv1) after treatment at concentrations of 0-10 μM for 48 h. The IC50 values were 0.78 μM, 1.07 μM, and 0.82 μM, respectively.TRIM24/BRPF1-IN-2 was also able to inhibit prostate cancer cells' gene and protein expression. In addition, TRIM24/BRPF1-IN-2 showed good Caco-2 permeability.
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Storage & Handling

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

Alternative Names

EpigeneticReaderDomain, Epigenetic Reader Domain, BRPF1

Compound Identifiers

PubChem CID

164946756