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GSK1324726A

Catalog No. T6021   CAS 1300031-52-0
Synonyms: I-BET726

GSK1324726A (I-BET726) is a greatly specific inhibitor of BET family proteins for BRD2(IC50=41 nM), BRD3(IC50=31 nM), and BRD4 (IC50=22 nM).

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GSK1324726A Chemical Structure
GSK1324726A, CAS 1300031-52-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 39.00
2 mg In stock $ 56.00
5 mg In stock $ 88.00
10 mg In stock $ 139.00
25 mg In stock $ 289.00
50 mg In stock $ 466.00
100 mg In stock $ 628.00
500 mg In stock $ 1,450.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 99.74%
Purity: 98.34%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK1324726A (I-BET726) is a greatly specific inhibitor of BET family proteins for BRD2(IC50=41 nM), BRD3(IC50=31 nM), and BRD4 (IC50=22 nM).
Targets&IC50 BRD4:22 nM, BRD2:41 nM, BRD3:31 nM
Kinase Assay Determination of BET Protein Binding Affinities to I-BET726: For determination of binding affinities to BET protein bromodomains, I-BET726 is titrated against truncates containing both BD1 and BD2 of BRD2 (10 nM), BRD3 (10 nM), and BRD4 (10 nM) in 50 mM HEPES pH7.5, 150 mM NaCl, 5% Glycerol, 1 mM DTT and 1 mM CHAPS in the presence of an Alexa 647 derivative (50 nM) of fluorescent ligand. After equilibrating for 1 h, the bromodomain protein: ligand interaction is detected using Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) following the addition of 1.5 nM europium chelate labeled anti-6His antibody. Plates are read using an Envision Plate reader (λEX = 337 nm, λEM = 615 nm, λEM = 665 nm; dual dichroic = 400 nm & 630 nm). These data are fitted to a four parameter IC50 model using Graphit data analysis software.
Cell Research Briefly, cells are seeded into 384-well or 96-well plates at a density optimized for 6 days of growth. The following day, T0 measurements are taken using CellTiter-Glo, CellTiter-Fluor, or CyQuant Direct, following the manufacturer's instructions. Plates are read on an Envision, Safire 2, or SpectraMax Gemini EM plate reader. Remaining plates are treated with DMSO or a titration of I-BET726. Cells are incubated for 6 days and developed as described above. Results are plotted as a percentage of the T0 value, normalized to 100%, versus concentration of compound. A 4-parameter equation is used to generate concentration response curves. Growth IC50 (gIC50) values are calculated at the mid-point of the growth window (between DMSO and T0 values). Ymin-T0 values are calculated by subtracting the T0 value (100%) from the Ymin value on the curve, and are a measure of net population cell growth or death.(Only for Reference)
Synonyms I-BET726
Molecular Weight 434.91
Formula C25H23ClN2O3
CAS No. 1300031-52-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (183.9 mM)

Ethanol: 80 mg/mL (183.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Wyce A, et al. PLoS One. 2013, 8(8), e72967. 2. Gosmini R, et al. J Med Chem. 2014, 57(19), 8111-8131.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Histone Modification Compound Library Anti-Aging Compound Library Inhibitor Library Kinase Inhibitor Library Chromatin Modification Compound Library Reprogramming Compound Library PPI Inhibitor Library

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Keywords

GSK1324726A 1300031-52-0 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain GSK-1324726A I-BET-726 Inhibitor I-BET726 inhibit I-BET 726 inhibitor

 

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