| 名称 | BRD4770 |
| 描述 | BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence. |
| 细胞实验 | 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) |
| 激酶实验 | 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. |
| 体内活性 | BRD4770和棉酚联用可以增加LC3-II水平和自噬体数量,从而协同作用诱导PANC-1细胞死亡。BRD4770在胰腺癌细胞系PANC-1中,通过通过抑制G9a降低二 - 和三甲基化H3K9的细胞水平,诱导衰老,并抑制贴壁依赖性和非依赖性增殖。 |
| 存储条件 | Store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : < 1.52 mg/mL (3.68 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+90% (20% SBE-β-CD in Saline) : < 1.52 mg/mL (3.68 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+90% Corn oil : 1.52 mg/mL (3.68 mM), Solution.
10% DMSO+90% Saline : < 1.52 mg/mL (3.68 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 15.15 mg/mL (36.64 mM), Sonication is recommended.
H2O : 10 mg/mL (24.19 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 0.5 mg/mL (1.21 mM), Sonication is recommended.
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| 关键字 | senescent | methylation | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | H3K9 | G9a | EHMT2 | chromatin | cell-permeable | BRD-4770 | BRD4770 | BRD 4770 | ATR | ATM | anti-proliferation |
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