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GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
| Molecular Weight | 410.44 |
| Formula | C23H23FN2O4 |
| CAS Number | 2138473-38-6 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Related Epigenetic Reader Domain Products |
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| RVX-208
Apabetalone (RVX-208) is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2. |
| I-BET151
I-BET151 (GSK1210151A) is an inhibitor of the BET family with IC50 of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively. |
| (+)-JQ1
(+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway. |
| I-BET-762
I-BET-762 (GSK525762) is a selective small molecule BET inhibitor. |
| CPI-0610
CPI-0610 is a novel BET protein bromodomain inhibitor. |
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