GSK1379725A (AU1) (Synonyms: AU1) |
| رقم الكتالوجGC30259 |
GSK1379725A عبارة عن رابط BPTF انتقائي مع Kd 2.8 uM ، ولا يظهر أي نشاط ملزم لـ Brd4
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Cas No.: 1802251-00-8
Sample solution is provided at 25 µL, 10mM.
GSK1379725A is an inhibitor of Brd4 and a selective BPTF ligand (Kd=2.8 μM).
From the NMR titration of GSK1379725A, the bound and unbound resonances are separated by 171 Hz, providing an upper bound for the chemical exchange rate. Assuming an association rate of 1×108 M-1 s-1 as a high end for a range of protein-small molecule interactions, (e.g., chymotrypsin: proflavin k1=1.2×108 M-1 s-1), an upper Kd of 8 μM is estimated from this experiment. For a more accurate determination with a non-fluorinated protein, ITC is used as a complementary direct binding assay using unlabeled BPTF. A Kd of 2.8 μM is obtained, consistent with our intermediate exchange resonance broadening by PrOF NMR. Although GSK1379725A has been demonstrated to be selective over Brd4, a full selectivity panel against other bromodomains will be needed. A database search using ChEMBL only showed GSK1379725A to be active in five cellular assays with an EC50 of 500 nM carried out. Additionally, no kinase activity has been reported for GSK1379725A despite the growing screening use of the PKIS library[1].
[1]. Urick AK, et al. Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules. ACS Chem Biol. 2015 Oct 16;10(10):2246-56.
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Cell experiment: |
Cell viability assay of HEK 293 cells are performed using resazurine dye based CellTiter-Blue. HEK 293T cells are plated in 96 well plates and experiments conducted when cells are 80% confluent. Cells are treated with the 0, 1.0, 3.0 and 10.0 μM GSK1379725A (AU1) for 24 and 48 hours in 5% CO2 (n=5-6, per condition). 20 μL of CellTiter-Blue is added to the each well and incubated for 2.5 h at 37°C. As resazurin dye is reduced by viable cells to resorufin. Resorufin is fluorescent at 580 excitation and 590 emission. The data is normalized with the control (DMSO treated)[1]. |
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References: [1]. Urick AK, et al. Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules. ACS Chem Biol. 2015 Oct 16;10(10):2246-56. |
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| Cas No. | 1802251-00-8 | SDF | |
| المرادفات | AU1 | ||
| Canonical SMILES | O=C(OC)C1=CC=CC(NC(NC2CN(C3=NC(NC4=CC=C(F)C=C4)=NC=C3)CC2)=O)=C1 | ||
| Formula | C23H23FN6O3 | M.Wt | 450.47 |
| الذوبان | DMSO: 83.33 mg/mL (184.98 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2199 mL | 11.0995 mL | 22.199 mL |
| 5 mM | 0.444 mL | 2.2199 mL | 4.4398 mL |
| 10 mM | 0.222 mL | 1.11 mL | 2.2199 mL |
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- Purity: >98.00%
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