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.
Tel
+86-530-529 6766,+86-15666160102 15666160102
Fax
0530-529 6766
Email
info@chuangli-chem.com
Country
China
ProdList
899
Advantage
55
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ:65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
7312
Advantage
58
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9806
Advantage
58
ShangHai Biochempartner Co.,Ltd
Tel
17754423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8011
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
21-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2998
Advantage
58
Shanghai SuperLan Chemcial Technique Centre
Tel
021-2022843681 15618226720
Fax
+86-21-51601218
Email
lucy@atkchemical.com
Country
China
ProdList
9987
Advantage
58
Twochem Co.Ltd.
Tel
021-58111628 15800915896
Fax
QQ 3285589261
Email
sales@twochem.com
Country
China
ProdList
1788
Advantage
58
Changzhou Extraordinary Pharmatech co., LTD.
Tel
+86-519-82111935 15195055733
Fax
051982611250
Email
info@feifanchem.com
Country
China
ProdList
362
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32161
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
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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