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BRD4770

Catalog No. T1923   CAS 1374601-40-7

BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.

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BRD4770 Chemical Structure
BRD4770, CAS 1374601-40-7
Pack Size Availability Price/USD Quantity
2 mg In stock $ 30.00
5 mg In stock $ 48.00
10 mg In stock $ 77.00
25 mg In stock $ 128.00
50 mg In stock $ 207.00
100 mg In stock $ 369.00
1 mL * 10 mM (in DMSO) In stock $ 53.00
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Purity: 99.82%
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Biological Description
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Description BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
Targets&IC50 G9a(EHMT2):5 μM
Kinase Assay 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 50 mM 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 50 mM 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 (50 mM 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 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)
Molecular Weight 413.47
Formula C25H23N3O3
CAS No. 1374601-40-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 8.3 mg/mL (20 mM)

TargetMolReferences and Literature

1. Yuan Y, et al. ACS Chem Biol. 2012, 7(7), 1152-1157. 2. Yuan Y, et al. Cell Death Dis. 2013, 4,e690.

Related compound libraries

This product is contained In the following compound libraries:
NO PAINS Compound Library Bioactive Compound Library Inhibitor Library Stem Cell Differentiation Compound Library Histone Modification Compound Library Methylation Compound Library Chromatin Modification Compound Library Anti-COVID-19 Compound Library Reprogramming Compound Library Anti-Aging Compound Library

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Keywords

BRD4770 1374601-40-7 Chromatin/Epigenetic Histone Methyltransferase EHMT2 G9a H3K9 cell-permeable ATR chromatin anti-proliferation methylation BRD-4770 Inhibitor ATM senescent inhibit BRD 4770 inhibitor

 

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