BRD-4770

SKU: orb1226419

Description

A SAM mimetic that selectively inhibits a subset of Histone Methyltransferase (HMTs), including G9a, in biochemical assays and in cells; decreases H3K9 trimethylation level in PANC-1 cells with EC50 of 5 uM; induces senescence, and inhibits both anchorage-dependent and -independent proliferation in PANC-1 cells; also increases LC3-II levels and the autophagosome number in PANC-1 cells combined with Gossypol.

Key Properties

• CAS Number: 1374601-40-7
• MW: 413.4684
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₃N₃O₃
• SMILES: O=C(C1=CC=C2C(N=C(NC(C3=CC=CC=C3)=O)N2CCCC4=CC=CC=C4)=C1)OC
• Target: HMTase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  BRD4770 (0-20 μM; 72 hours; PANC-1 cells) treatment reduces the number of cells after 72 h. BRD4770 (2.5-5 μM; 24 hours; PANC-1 cells) treatment decreases H3K9 trimethylation level by 23% in PANC-1 cells. BRD4770 induces a senescent phenotype in a pancreatic cancer cell line. BRD4770 also inhibits both anchorage-dependent and -independent cell proliferation and induces G2/M cell-cycle arrest. BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway without inducing DNA damage, while the ataxia telangiectasia and Rad3-related protein (ATR) pathway is not affected. BRD4770 also induces increased levels of lysine acetylation in cells without inhibiting histone deacetylases. Cell Viability Assay Cell line: PANC-1 cells. Concentration: 0 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM Incubation time: 72 hours. Result: Reduced the number of cells after 72 h. Western blot analysis. Cell line: PANC-1 cells. Concentration: 2.5 μM, 5 μM Incubation time: 24 hours. Result: Decreased H3K9 trimethylation level by 23% in PANC-1 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRD 4770 | BRD4770

Quick Database Links

Gene Symbol

HMTase