| Name | GSK620 |
| 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 |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (10.14 mM), Sonication is recommended.
DMSO : 45 mg/mL (138.31 mM), Sonication is recommended.
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| Keywords | whole | selectivity | phenotype | pan-BD2 | oral | Inhibitor | inhibit | human | GSK-620 | GSK620 | GSK 620 | EpigeneticReaderDomain | Epigenetic Reader Domain | blood | anti-inflammatory |
| Inhibitors Related | ABBV-744 | SNDX-5613 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | 5-Ph-IAA | Curcumin | dBET6 | Naphthol AS-E | JQ-1 (carboxylic acid) | Bisdemethoxycurcumin |
| Related Compound Libraries | Reprogramming Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | PPI Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
