For research use only. Not for therapeutic Use.
GSK620 is a potent and orally active pan-BD2 inhibitor 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[1].
GSK620 shows an anti-inflammatory phenotype in human whole blood. 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[1].
Highlighting the utility of GSK620 as an in vivo tool, efficacy is observed in separate models of inflammatory arthritis, psoriasis, and hepatitis[1].
| Catalog Number | I028391 |
| CAS Number | 2088410-46-0 |
| Synonyms | 1-benzyl-5-N-cyclopropyl-3-N-methyl-2-oxopyridine-3,5-dicarboxamide |
| Molecular Formula | C18H19N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C18H19N3O3/c1-19-17(23)15-9-13(16(22)20-14-7-8-14)11-21(18(15)24)10-12-5-3-2-4-6-12/h2-6,9,11,14H,7-8,10H2,1H3,(H,19,23)(H,20,22) |
| InChIKey | QZZCUOVXHPAQRQ-UHFFFAOYSA-N |
| SMILES | CNC(=O)C1=CC(=CN(C1=O)CC2=CC=CC=C2)C(=O)NC3CC3 |
| Reference | [1]. Seal JT, et al. The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor. J Med Chem. 2020;63(17):9093-9126. |
