化合物GSK1379725A T15424

Product Introduction
Bioactivity


英文名: GSK1379725A

描述: GSK1379725A 是一种选择性 BPTF 配体，Kd 为 2.8 μM。

体外活性: 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 (EC50: 500 nM) carried out. Additionally, no kinase activity has been reported for GSK1379725A despite the growing screening use of the PKIS library[1]. 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.

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

溶解度: DMSO : 50 mg/mL (111 mM)


关键字: inhibit | Inhibitor | GSK1379725A | Epigenetic Reader Domain | GSK-1379725A

相关产品: CBP/EP300-IN-1 | PROTAC BET Degrader-1 | IACS-9571 Hydrochloride (1800477-30-8 free base) | E-7386 | HJB97 | ZL0454 | MS402 | GSK046 | dCBP-1 | Phoenixin-20 TFA

相关库: Bioactive Compounds Library Max | Epigenetics Compound Library | Covalent Inhibitor Library | Histone Modification Compound Library | Bioactive Compound Library

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