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GSK1379725A
🥰Excellent
Catalog No. T15424Cas No. 1802251-00-8
GSK1379725A is a selective BPTF ligand [Kd = 2.8 μM].
GSK1379725A
🥰Excellent
Purity: 99.59%
Catalog No. T15424Cas No. 1802251-00-8
GSK1379725A is a selective BPTF ligand [Kd = 2.8 μM].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $67 | In Stock | |
| 5 mg | $118 | In Stock | |
| 10 mg | $198 | In Stock | |
| 25 mg | $353 | In Stock | |
| 50 mg | $494 | In Stock | |
| 100 mg | $696 | In Stock | |
| 200 mg | $938 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $136 | In Stock |
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Purity:99.59%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Smiles | COC(=O)c1cccc(NC(=O)NC2CCN(C2)c2ccnc(Nc3ccc(F)cc3)n2)c1 |
| Relative Density. | 1.39 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (111 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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