Product Details
| Product Name:
GSK1379725A |
CAS No.:
1802251-00-8 |
| Purity:
99.59% |
Supply Ability:
10g |
| Release date:
2025/07/25 |
Product Introduction
Bioactivity
| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (111 mM), Sonication is recommended.
|
| Keywords | Inhibitor | inhibit | GSK-1379725A | GSK1379725A | EpigeneticReaderDomain | Epigenetic Reader Domain | BPTF |
| Inhibitors Related | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | CTB | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin |
| Related Compound Libraries | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Covalent Inhibitor Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States