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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 | Price | Availability | Quantity |
---|---|---|---|
5 mg | 41 € | In Stock | |
10 mg | 67 € | In Stock | |
25 mg | 135 € | In Stock | |
50 mg | 202 € | In Stock | |
100 mg | 304 € | In Stock | |
200 mg | 425 € | In Stock | |
1 mL x 10 mM (in DMSO) | 45 € | In Stock |
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 |
In vitro | In the mouse models SK-N-AS and CHP-212, GSK1324726A administered at 15 mg/kg orally (o.p.) was effective in inhibiting tumor growth and downregulating the expression of MYCN and BCL2. Additionally, at a dosage of 10 mg/kg intravenously (i.v.), GSK1324726A demonstrated potent anti-inflammatory effects and prevented mortality in mice experiencing septic shock. |
In vivo | In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. It regulates the expression of genes in the MYC family pathway, including direct expression of BCL2 and MYCN. |
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) |
Alias | I-BET726 |
Molecular Weight | 434.91 |
Formula | C25H23ClN2O3 |
Cas No. | 1300031-52-0 |
Smiles | C(C)(=O)N1C=2C([C@H](NC3=CC=C(Cl)C=C3)C[C@@H]1C)=CC(=CC2)C4=CC=C(C(O)=O)C=C4 |
Relative Density. | 1.304 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (114.97 mM) Ethanol: 80 mg/mL (183.9 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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