Chromatin/Epigenetic Epigenetic Reader Domain 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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Purity 99.63%
Purity 98.86%
Purity 98.00%
Purity 99.03%
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 ,   BRD3 ,   BRD4
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
Synonyms GSK1210151A
Purity 99.63%
Molecular Weight 415.44
Formula C23H21N5O3
CAS No. 1300031-49-5


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 )


References and Literature
1. Dawson MA, et al. Nature, 2011, 478(7370), 529-533. 2. Xiong C, Deng J, Wang X, et al. Pharmacologic Targeting of BET Proteins Attenuates Hyperuricemic Nephropathy in Rats[J]. Frontiers in Pharmacology. 2021, 12: 147. 3. Maksylewicz A, Bysiek A. BET bromodomain inhibitors suppress inflammatory activation of gingival fibroblasts and epithelial cells from periodontitis patients[J]. Frontiers in Immunology. 2019 Apr 30;10:933.

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 Kinase Inhibitor Library Anti-aging Compound Library Chromatin Modification Compound Library PPI Inhibitors Library

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