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GSK1379725A (AU1) Sale

(Synonyms: AU1) 目录号 : GC30259

GSK1379725A是Brd4的抑制剂,并且是BPTF的选择性配体(Kd=2.8μM)。

GSK1379725A (AU1) Chemical Structure

Cas No.:1802251-00-8

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5mg
¥4,016.00
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10mg
¥6,426.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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].

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.

产品描述

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.

Chemical Properties

Cas No. 1802251-00-8 SDF
别名 AU1
Canonical SMILES O=C(OC)C1=CC=CC(NC(NC2CN(C3=NC(NC4=CC=C(F)C=C4)=NC=C3)CC2)=O)=C1
分子式 C23H23FN6O3 分子量 450.47
溶解度 DMSO: 83.33 mg/mL (184.98 mM) 储存条件 Store at -20°C
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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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