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I-BET151

I-BET151
I-BET151 (GSK1210151A) (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).
Catalog No. T2120Cas No. 1300031-49-5
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Purity:99.63%
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I-BET151

Catalog No. T2120Cas No. 1300031-49-5
I-BET151 (GSK1210151A) (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$41In Stock
2 mg$59In Stock
5 mg$97In Stock
10 mg$117In Stock
25 mg$213In Stock
50 mg$357In Stock
100 mg$533In Stock
500 mg$1,190In Stock
1 mL x 10 mM (in DMSO)$107In Stock
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Product Introduction

Bioactivity
Description
I-BET151 (GSK1210151A) (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).
Targets&IC50
BRD3:0.25 μM, BRD4:0.79 μM, BRD2:0.5 μM
In vitro
I-BET151 administration (30 mg/kg/day) in mice significantly inhibits the growth of MLL-AF9 murine and MLL-AF4 human leukemia tumors and notably prolongs lifespan.
In vivo
When interacting with HL60 nuclear extracts, I-BET151 at concentrations of 0.5 or 5 μM inhibits the binding of BETs (BRD2/3/4/9) to acetylated histone peptides without affecting 23 other bromodomain proteins. This compound demonstrates potent inhibitory effects on cell lines with various MLL fusions, such as MV4;11, RS4;11, MOLM13, and NOMO1 cells (IC50: 15-192 nM). I-BET151 shows broad selectivity in inhibiting multiple protein types, including COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, and transporters. Similar to I-BET762 (GSK525762A), I-BET151 possesses a high binding affinity for BRD2/3/4 (Kd: 0.02-0.1 μM) and significantly inhibits the production of the IL-6 cytokine in response to lipopolysaccharide stimulation in human peripheral blood mononuclear cells, whole blood, and rat WB (IC50: 0.16/1.26/1.26 μM).
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)
AliasGSK1210151A
Chemical Properties
Molecular Weight415.44
FormulaC23H21N5O3
Cas No.1300031-49-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (120.35 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4071 mL12.0354 mL24.0709 mL120.3543 mL
5 mM0.4814 mL2.4071 mL4.8142 mL24.0709 mL
10 mM0.2407 mL1.2035 mL2.4071 mL12.0354 mL
20 mM0.1204 mL0.6018 mL1.2035 mL6.0177 mL
50 mM0.0481 mL0.2407 mL0.4814 mL2.4071 mL
100 mM0.0241 mL0.1204 mL0.2407 mL1.2035 mL

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