Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 33.00 | |
5 mg | In stock | $ 76.00 | |
10 mg | In stock | $ 122.00 | |
25 mg | In stock | $ 247.00 | |
50 mg | In stock | $ 396.00 | |
100 mg | In stock | $ 589.00 | |
500 mg | In stock | $ 1,280.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 84.00 |
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 | 325.36 |
Formula | C18H19N3O3 |
CAS No. | 2088410-46-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 62.5 mg/mL (192.09 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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GSK620 2088410-46-0 Chromatin/Epigenetic Epigenetic Reader Domain Inhibitor oral phenotype selectivity whole anti-inflammatory GSK-620 inhibit human GSK 620 blood inhibitor