BRD4770

Catalog No.S7591

For research use only.

BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.

BRD4770 Chemical Structure

CAS No. 1374601-40-7

Selleck's BRD4770 has been cited by 3 Publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.
Targets
G9a [1]
()
In vitro

BRD4770 reduces cellular levels of di- and trimethylated H3K9 via inhibition of G9a, induces senescence, and inhibits both anchorage-dependent and -independent proliferation in the pancreatic cancer cell line PANC-1. [1] The combination of gossypol and BRD4770 increases LC3-II levels and the autophagosome number, and thus acts in synergy to induce cell death in PANC-1 cells. [2]

Protocol (from reference)

Kinase Assay:[1]
  • Biochemical activity of G9a:

    Dissociation Enhanced Lanthanide Fluoro-ImmunoAssays (DELFIA) are performed in white, opaque 384-well plates coated with Neutravidin. Test compounds are diluted to 12 μg/mL in 50mM Tris-HCl pH 8.5 containing 4% DMSO and 10 μL is dispensed into the wells. Blank and control wells received only compound buffer. GST-G9a at 10 μg/mL and SAM at 40 μM are diluted in 50mM Tris HCl pH 8.5/10 mM DTT and added in a volume of 20 μL. Blank wells receives Tris/DTT buffer only. The reactions are initiated by the addition of 800 nM H3(1-20)-cysbiotin substrate in 50 mM Tris pH 8.5 in a volume of 10 μl, and incubated at room temperature for 60 minutes. The plates are washed 3 times with 100 μl of Wash Buffer (50mM Tris pH 7.4, 150 mM NaCl, 0.05% Tween 20, 0.2% BSA). Next, 50 μl of Fluoroimmunoassay (FI) Buffer (50 mM Tris HCl pH 7.8, 150 mM NaCl, 0.05% Tween 40, 25 μM DTPA, 0.2% BSA, 0.05% BGG) containing 5ng α-2X-di-meth H3-K9 and 5ng goat anti-rabbit Eu chelate is added to all wells of the plate, and the plate is incubated for an additional hour at room temperature. The plates are washed 3 times with 100 μL of Wash Buffer, and 50 μL of Enhancement Solution is added to each well. Time resolved fluorescence is measured after 45 minutes on a Viewlux Microplate Imager imaging for 15 seconds with a 354 μs window, 400 μs delay, excitation at 360 nm, and emission at 618 nm.

Cell Research:[1]
  • Cell lines: PANC-1 cells
  • Concentrations: ~20 μM
  • Incubation Time: 72 hours
  • Method: 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.

Solubility (25°C)

In vitro

DMSO 27 mg/mL warmed
(65.3 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 413.47
Formula

C25H23N3O3

CAS No. 1374601-40-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC(=O)C1=CC2=C(C=C1)N(C(=N2)NC(=O)C3=CC=CC=C3)CCCC4=CC=CC=C4

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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