[CAS NO. 2474876-09-8] GSK046
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PRODUCTS SPECIFICATIONS [2474876-09-8]
Store
Catalog
SLK-S9684
Brand
Selleck
CAS
2474876-09-8
DESCRIPTION [2474876-09-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 414.47 |
| Molecular Formula | C23H27FN2O4 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4127 mL | 12.0636 mL | 24.1272 mL |
| 5 mM | 0.4825 mL | 2.4127 mL | 4.8254 mL |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4127 mL |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4825 mL |
Description
GSK046 (iBET-BD2) is a selective and orally active inhibitor of with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2, BRD3, BRD4 and BRDT, respectively. GSK046 exhibits immunomodulatory activity.
Targets
In vitro
GSK046 shows an excellent level of selectivity for the BET family with no measurable activity for non-BET bromodomains. GSK046 is tested in an LPS-stimulated peripheral blood mononuclear cell (PBMC) cellular assay. After stimulation, these immune cells release a range of cytokines and chemokines, including monocyte chemoattractant protein 1 (MCP-1/CCL2). GSK046 also inhibits MCP-1 production (pIC50 = 7.5) with a minimal drop-off from the biochemical BRD4 BD2 potency observed.
References
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