GSK-340 |CAS:2222509-79-5 Probechem Biochemicals

Chemical Structure : GSK-340

GSK-340 (GSK340;GSK 340)

Catalog No.: PC-63487Not For Human Use, Lab Use Only.

GSK-340 is a potent, selective inhibitor of second bromodomains of the BET family (BD2) with pKd of 8.18, 7.49, 7.72 and 7.68 for BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2, respectively.

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Biological Activity

GSK-340 is a potent, selective inhibitor of second bromodomains of the BET family (BD2) with pKd of 8.18, 7.49, 7.72 and 7.68 for BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2, respectively.
GSK-340 displays 229-, 40-, 48- and 91-fold selectivity over the responding BD1, >100-fold selectivity over TAF1, WRD9, ATAD2A/B and other bromodomains (pKd<5.0).
GSK-340 inhibits BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2 with pIC50 of 7.2, 6.5, 7.3 and 6.7, respectively.
GSK-340 inhibits release of the MCP-1 cytokine in human PBMCs (pIC50=7.4) and whole blood.
GSK-340 is an useful in vitro tool molecule for investigation into the biological role of the BD2 domains.

Physicochemical Properties

M.Wt	417.553
Formula	C26H31N3O2
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	(S)-1-(2-cyclopropyl-4-(2-(hydroxymethyl)benzyl)-6-(1,2,3,6-tetrahydropyridin-4-yl)-3,4-dihydroquinoxalin-1(2H)-yl)ethan-1-one

References

1. Law RP, et al. J Med Chem. 2018 May 3. doi: 10.1021/acs.jmedchem.7b01666.

GSK-340 (GSK340;GSK 340)

Biological Activity

Physicochemical Properties

References

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