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

China 43 United States 4 Global 47

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: 9805
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: 2951
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
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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

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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)-

GSK620, 10 mM in DMSO

2088410-46-0

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