GSK620
- Product Name
- 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
- Formula Weight
- 325.36
- MOL File
- 2088410-46-0.mol
GSK620 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0142650
- Product name
- GSK620
- Purity
- 99.86%
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CS-0142650
- Product name
- GSK620
- Purity
- 99.86%
- Packaging
- 10mg
- Price
- $480
- Updated
- 2021/12/16
- Product number
- CS-0142650
- Product name
- GSK620
- Purity
- 99.86%
- Packaging
- 25mg
- Price
- $950
- Updated
- 2021/12/16
- Product number
- CS-0142650
- Product name
- GSK620
- Purity
- 99.86%
- Packaging
- 50mg
- Price
- $1450
- Updated
- 2021/12/16
- Product number
- CS-0142650
- Product name
- GSK620
- Purity
- 99.86%
- Packaging
- 100mg
- Price
- $2250
- Updated
- 2021/12/16
GSK620 Chemical Properties,Usage,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
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View Lastest Price from GSK620 manufacturers
- Product
- GSK620 2088410-46-0
- Price
- US $1.00/box
- Min. Order
- 1box
- Purity
- 98%
- Supply Ability
- 1
- Release date
- 2022-11-19