| Name | GSK1379725A |
| Description | GSK1379725A is a selective BPTF ligand [Kd = 2.8 μM]. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (111 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.44 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | GSK-1379725A | GSK1379725A | EpigeneticReaderDomain | Epigenetic Reader Domain | BPTF |
| Inhibitors Related | ABBV-744 | SNDX-5613 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | 5-Ph-IAA | Curcumin | dBET6 | Naphthol AS-E | JQ-1 (carboxylic acid) | Bisdemethoxycurcumin |
| Related Compound Libraries | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Covalent Inhibitor Library | Anti-Cancer Compound Library |
United States
