GSK973
Product Specifications
CAS Number
2138473-38-6
Target
Epigenetic Reader Domain, Others
Related Pathways
Others, Chromatin/Epigenetic
Bioactivity
GSK973 is a highly selective and orally bioavailable inhibitor that targets the second bromodomains (BD2s) of the BET family. It exhibits a pIC 50 of 7.8 and a pK d of 8.7 specifically for BRD4 BD2. Additionally, GSK973 demonstrates a remarkable selectivity of 1600-fold for BRD4 BD2 over BRD4 BD1. Moreover, it displays good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC 50 ranging from 7.4 to 7.8 and pK d ranging from 8.3 to 8.5.
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[H][C@@]12COC[C@]1([H])[C@H]2NC(=O)c1cc2[C@@H]([C@@H](CF)Oc2c(c1)C(=O)NC)c1ccccc1
Molecular Formula
C23H23FN2O4
Molecular Weight
410.445
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
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