BRD4770

SKU: orb1307100

Description

BRD4770 is a cell-permeable small molecule inhibitor of the histone methyltransferase G9a (EHMT2). It induces cellular senescence and has been used in vitro to study epigenetic regulation in cancer, aging, and cellular reprogramming research.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1374601-40-7
• MW: 413.47
• Purity: 99.82% (May vary between batches)
• Formula: C₂₅H₂₃N₃O₃
• SMILES: COC(=O)c1ccc2n(CCCc3ccccc3)c(NC(=O)c3ccccc3)nc2c1
• Target: Histone Methyltransferase
• Solubility: DMSO:15.15 mg/mL (36.64 mM);H2O:10 mg/mL (24.19 mM);10% DMSO+90% Corn Oil:0.5 mg/mL (1.21 mM)

Bioactivity

• Target IC50:
  G9a/EHMT2:5 μM
• In Vivo:
  When used in conjunction with cotinine, BRD4770 increases the levels of LC3-II and the number of autophagosomes, thereby synergistically inducing cell death in the PANC-1 pancreatic cancer cell line. In these cells, BRD4770 induces senescence and inhibits both adhesion-dependent and -independent proliferation by suppressing G9a, which leads to a reduction in the cellular levels of di- and trimethylated H3K9.
• Cell Research:
  PANC-1 cells are seeded and treated with BRD4770 in 6-well plates for 72 h. Cells are trypsinized and tested for soft agar colony formation using CytoSelect 96-Well Cell Transformation Assay, using the CyQuant GR dye to measure total cellular nucleic acid levels. Fluorescence is detected with an Analyst HT plate reader using a 485/520 nm filter set.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, methylation, EHMT2, G9a, H3K9, Inhibitor, HistoneMethyltransferase, Histone Methyltransferase, anti-proliferation, ATM, ATR, cell-permeable, BRD4770, BRD-4770, chromatin, BRD 4770, senescent

Compound Identifiers

PubChem CID

72193870