GSK620
- CAS No.
- 2088410-46-0
- Chemical Name:
- GSK620
- Synonyms
- GSK620;GSK620, 10 mM in DMSO;1-benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide;3,5-Pyridinedicarboxamide, N5-cyclopropyl-1,2-dihydro-N3-methyl-2-oxo-1-(phenylmethyl)-;Inhibitor,oral,GSK 620,phenotype,selectivity,GSK-620,whole,anti-inflammatory,GSK620,Epigenetic Reader Domain,inhibit,human,blood
- CBNumber:
- CB48067227
- Molecular Formula:
- C18H19N3O3
- Molecular Weight:
- 325.36
- MDL Number:
- MFCD32899274
- MOL File:
- 2088410-46-0.mol
| Product description | Number | Pack Size | Price |
| GSK620 99.86% | CS-0142650 | 5mg | $300 |
| GSK620 99.86% | CS-0142650 | 10mg | $480 |
| GSK620 99.86% | CS-0142650 | 25mg | $950 |
| GSK620 99.86% | CS-0142650 | 50mg | $1450 |
| GSK620 99.86% | CS-0142650 | 100mg | $2250 |
| 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) |
| form | Solid |
| color | White to off-white |
| 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 | C1(=O)N(CC2=CC=CC=C2)C=C(C(NC2CC2)=O)C=C1C(NC)=O |
| UNSPSC Code | 51111800 |
| NACRES | NA.77 |
GSK620 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0142650 | GSK620 99.86% | 2088410-46-0 | 5mg | $300 | 2021-12-16 | Buy |
| ChemScene | CS-0142650 | GSK620 99.86% | 2088410-46-0 | 10mg | $480 | 2021-12-16 | Buy |
| ChemScene | CS-0142650 | GSK620 99.86% | 2088410-46-0 | 25mg | $950 | 2021-12-16 | Buy |
| ChemScene | CS-0142650 | GSK620 99.86% | 2088410-46-0 | 50mg | $1450 | 2021-12-16 | Buy |
| ChemScene | CS-0142650 | GSK620 99.86% | 2088410-46-0 | 100mg | $2250 | 2021-12-16 | Buy |
GSK620 Chemical Properties,Uses,Production
Uses
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].
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].
in vitro
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.
in vivo
Highlighting the utility of GSK620 as an in vivo tool, efficacy is observed in separate models of inflammatory arthritis, psoriasis, and hepatitis.
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
Raw materials
Preparation Products
GSK620 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32434 | 58 |
| Wuhan Nutra Biotechnology Co.,Ltd | +8617786394783 | nutrabiotech@outlook.com | China | 300 | 58 |
| Shenzhen Shengda Pharma Limited | 755-85269922 +8613424394241 | sales@shengdapharm.com | CHINA | 310 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39032 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| HANGZHOU LEAP CHEM CO., LTD. | +86-571-87711850 | market18@leapchem.com | China | 43339 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 |
