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GSK620

Chemical Structure : GSK620

CAS No.: 2088410-46-0

GSK620 (GSK-620)

Catalog No.: PC-72179Not For Human Use, Lab Use Only.

GSK620 (GSK-620) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.1 (BRD4 BD2), 220-fold selectivity over BD1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK620 (GSK-620) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.1 (BRD4 BD2), 220-fold selectivity over BD1.
GSK620 significantly and dose-dependently inhibited both the arthritic score and IgG1 production in response to the immunisation in collagen-induced arthritis model in rats, showed similar level of efficacy to the pan-BET inhibitor I-BET151 and also dramatically reduced joint swelling, synovitis, cartilage damage, pannus formation and bone resorption.

Physicochemical Properties

M.Wt 325.37
Formula C18H19N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-Benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide

References

1. Gilan O, et al. Science. 2020 Apr 24;368(6489):387-394.

2. Seal JT, et al. J Med Chem. 2020 Sep 10;63(17):9093-9126.

3. Aylott HE, et al. J Med Chem. 2021 Mar 25;64(6):3249-3281.

4. Rianjongdee F, et al. J Med Chem. 2021 Aug 12;64(15):10806-10833.

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