GSK620

Product Name: GSK620
CAS No.: 2088410-46-0
Chemical Name: GSK620
Synonyms: GSK620;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

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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)

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0142650
Product name: GSK620
Purity: 99.86%
Packaging: 5mg
Price: $300
Updated: 2021/12/16

ChemScene

Product number: CS-0142650
Product name: GSK620
Purity: 99.86%
Packaging: 10mg
Price: $480
Updated: 2021/12/16

ChemScene

Product number: CS-0142650
Product name: GSK620
Purity: 99.86%
Packaging: 25mg
Price: $950
Updated: 2021/12/16

ChemScene

Product number: CS-0142650
Product name: GSK620
Purity: 99.86%
Packaging: 50mg
Price: $1450
Updated: 2021/12/16

ChemScene

Product number: CS-0142650
Product name: GSK620
Purity: 99.86%
Packaging: 100mg
Price: $2250
Updated: 2021/12/16

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GSK620 Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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GSK620 Suppliers

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View Lastest Price from GSK620 manufacturers

Wuhan Nutra Biotechnology Co.,Ltd

Product: GSK620 2088410-46-0
Price: US $1.00/box
Min. Order: 1box
Purity: 98%
Supply Ability: 1
Release date: 2022-11-19

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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)-

2088410-46-0

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