Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL (183.9 mM)
Ethanol: 80 mg/mL (183.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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GSK1324726A 1300031-52-0 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain GSK-1324726A I-BET-726 Inhibitor I-BET726 inhibit I-BET 726 inhibitor