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Chromatin/Epigenetic Epigenetic Reader Domain I-BET151

I-BET151

Catalog No. T2120   CAS 1300031-49-5
Synonyms: GSK1210151A

I-BET151 (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).

I-BET151, CAS 1300031-49-5
Pack Size Availability Price/USD Quantity
2 mg In stock 74.00
5 mg In stock 120.00
10 mg In stock 140.00
25 mg In stock 300.00
50 mg In stock 430.00
100 mg In stock 750.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description I-BET151 (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).
Targets&IC50 BRD2 :ic50 0.5μM,   BRD3 :ic50 0.25μM,   BRD4 :ic50 0.79μM,  
Kinase Assay Fluorescence anisotropy (FP) ligand displacement assay: All components are dissolved in buffer of composition 50 mM HEPES pH 7.4, 150 mM NaCl and 0.5 mM CHAPS with final concentrations of BRD 2/3/4 75 nM, fluorescent ligand 5 nM. 10 μL of this reaction mixture is added using a micro multidrop to wells containing 100 nL of various concentrations of I-BET151 or DMSO vehicle (1% final) in Greiner 384 well Black low volume microtitre plate and equilibrated in the dark for 60 minutes at room temperature. Fluorescence anisotropy is read in Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM).
Cell Research
Cells are exposed to various concentrations of I-BET151 for 24 or 72 hours in 384-well or 96-well plates. For cell growth inhibition assays, plates are added with CellTiter-Glo reagent using a volume equivalent to the cell culture volume in the wells, shaken for approximately 2 minutes and chemiluminescent signal is read on the Analyst GT or EnVision Plate Reader. For cell proliferation assays, CellTiter-Aqueous One is added to each well and plates are incubated for 4 hours at 37 °C. Absorbance is read at 490 nm on a SpectraMax Gemini reader (Only for Reference)
Cell lines: MV4;11, MOLM13, NOMO1, RS4;11, HEL, HL60 and K562
Animal Research
Animal Model: NOD-SCID mice injected intravenously with MV4;11 cells, and C57BL/6 mice injected intravenously with MLL-AF9 cells
Synonyms GSK1210151A
Purity 99.63%
Molecular Weight 415.44
Formula C23H21N5O3
CAS No. 1300031-49-5

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 199.8 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Dawson MA, et al. Nature, 2011, 478(7370), 529-533.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Stem cell Differentiation Compound Library Epigenetics Compound Library Histone Modification Research Compound Library

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