Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK1379725A is a selective BPTF ligand (Kd = 2.8 μM).
説明 | GSK1379725A is a selective BPTF ligand (Kd = 2.8 μM). |
ターゲット&IC50 | BPTF:2.8 μM(Kd) |
In vitro | GSK1379725A has proven to be selective towards Brd4, though comprehensive evaluation against other bromodomains is necessary. Searches in the ChEMBL database reveal its activity in only five cellular assays, indicating a potency (EC50) of 500 nM, with no kinase activity noted despite extensive screenings, especially with the PKIS library[1]. NMR titration data showed a separation of 171 Hz between bound and unbound resonances of GSK1379725A, suggesting a maximum chemical exchange rate. Based on an assumed high association rate (e.g., similar to chymotrypsin: proflavin at 1.2×108 M-1 s-1), the dissociation constant (Kd) is approximately 8 μM. For more precise Kd measurement, ITC was employed with unlabeled BPTF, yielding a Kd of 2.8 μM, aligning with the observed intermediate exchange resonance broadening detected by PrOF NMR, thus confirming the specificity and binding characteristics of GSK1379725A. |
分子量 | 450.47 |
分子式 | C23H23FN6O3 |
CAS No. | 1802251-00-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (111 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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GSK1379725A 1802251-00-8 Chromatin/Epigenetic Epigenetic Reader Domain inhibit Inhibitor GSK-1379725A inhibitor