Description
| Description | GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood. |
| In vitro | GSK620 showed an anti-inflammatory phenotype in human whole blood, confirming it cellular target engagement.?Human blood samples are stimulated with LPS, which produces a strong immune response. The monocyte chemattractant protein 1 (MCP-1/CCL2) is measured. This is a chemokine which recruits monocytes, memory T cells, and dendritic cells to sites of inflammation. GSK620 reduces the MCP-1 response in a concentration-dependent manner with (an expected) ～1 log drop off in potency relative to the biochemical BRD4 BD2 potencies observed |
| Molecular Weight |
325.4 |
| Formula | C18H19N3O3 |
| CAS No. | 2088410-46-0 |
Storage
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Solubility Information
DMSO: 62.5 mg/mL (192.09 mM),
Need ultrasonic
( < 1 mg/ml refers to the product slightly soluble or insoluble )
