A BD2 bromodomain inhibitor
iBET-BD2 is an inhibitor of the bromodomain and extra-terminal domain (BET) family protein bromodomain 2 (BD2).1 It inhibits BD2 in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (IC50s = 264, 98, 49, and 214 nM, respectively) and is selective for BD2 over BD1 (IC50s = 10.96, 36.31, 70.55, and >50.11 ?M for BRD2, BRD3, BRD4, and BDT, respectively) in a time-resolved FRET (TR-FRET) assay. iBET-BD2 (1 ?M) inhibits IFN-γ-induced protein expression of MHC class I in K562 cells. It reduces the production of anti-KLH IgM antibodies in mice immunized with keyhole limpet hemocyanin (KLH) when administered at a dose of 40 mg/kg.
1.Gilan, O., Rioja, I., Knezevic, K., et al.Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammationScience368(6489)387-394(2020)
动态评分
0.0