ChemicalBook > CAS DataBase List > GSK620

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
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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)
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
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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].

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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GSK620 Suppliers

Heze Development Zone chuangli Chemical Co., Ltd.
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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

2088410-46-0, GSK620Related Search:


  • 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)-
  • GSK620, 10 mM in DMSO
  • 2088410-46-0
  • API