GSK620 manufacturers
- GSK620
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- $1.00/ box
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2022-11-21
- CAS:2088410-46-0
- Min. Order: 1box
- Purity: 98%
- Supply Ability: 1
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| Product Name: | GSK620 | | Synonyms: | GSK620;1-benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide;Inhibitor,oral,GSK 620,phenotype,selectivity,GSK-620,whole,anti-inflammatory,GSK620,Epigenetic Reader Domain,inhibit,human,blood;3,5-Pyridinedicarboxamide, N5-cyclopropyl-1,2-dihydro-N3-methyl-2-oxo-1-(phenylmethyl)- | | CAS: | 2088410-46-0 | | MF: | C18H19N3O3 | | MW: | 325.36 | | EINECS: | | | Product Categories: | API | | Mol File: | 2088410-46-0.mol |  |
| | GSK620 Chemical Properties |
| Boiling point | 618.6±55.0 °C(Predicted) | | density | 1.30±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 62.5 mg/mL (192.09 mM; Need ultrasonic) | | pka | 12.43±0.20(Predicted) |
| | GSK620 Usage And Synthesis |
| Biological Activity | 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]. | | References | [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. |
| | GSK620 Preparation Products And Raw materials |
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