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Chemical Structure : 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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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.
| M.Wt | 417.553 | |
| Formula | C26H31N3O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Law RP, et al. J Med Chem. 2018 May 3. doi: 10.1021/acs.jmedchem.7b01666.
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