product name BRD4770
Description: BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence. BRD4770 reduced cellular levels of di- and trimethylated H3K9 without inducing apoptosis, induced senescence, and inhibited both anchorage-dependent and -independent proliferation in the pancreatic cancer cell line PANC-1. BRD4770 may be a useful tool to study G9a and its role in senescence and cancer cell biology.
References: ACS Chem Biol. 2012 Jul 20;7(7):1152-7; Cell Death Dis. 2013 Jun 27;4:e690.
413.47
Formula
C25H23N3O3
CAS No.
1374601-40-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 27 mg/mL (65.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. 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. Kinase Assay: 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 Assay: 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. |
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| In Vivo | |
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| Formulation & Dosage | |
| References | ACS Chem Biol. 2012 Jul 20;7(7):1152-7; Cell Death Dis. 2013 Jun 27;4:e690. |
