Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK1379725A is a selective BPTF ligand (Kd = 2.8 μM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 112.00 | |
5 mg | In stock | $ 197.00 | |
10 mg | In stock | $ 347.00 | |
25 mg | In stock | $ 589.00 | |
50 mg | In stock | $ 842.00 | |
100 mg | In stock | $ 1,160.00 | |
500 mg | In stock | $ 2,330.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 226.00 |
Description | GSK1379725A is a selective BPTF ligand (Kd = 2.8 μM). |
Targets&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. |
Molecular Weight | 450.47 |
Formula | C23H23FN6O3 |
CAS No. | 1802251-00-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 83.33 mg/mL (184.98 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GSK1379725A 1802251-00-8 Chromatin/Epigenetic Epigenetic Reader Domain inhibit Inhibitor GSK-1379725A inhibitor