BRD4 degrader-3 is a molecular glue degrader targeting BRD4, with binding activity towards the BD1 and BD2 domains of BRD4. BRD4 degrader-3 regulates the activity of BRD4. BRD4 degrader-3 inhibits MYC expression in cancer cells. BRD4 degrader-3 suppresses cell proliferation. BRD4 degrader-3 can be used in research related to acute myeloid leukemia and prostate cancer [1].
In Vitro, BRD4 degrader-3 (6 days) inhibits the proliferation of PC-3-STEAP-1 and EoL-1 cells, with IC50 values of 6.6 nM and 2.2 nM, respectively[1]. BRD4 degrader-3 (4 h) affects MYC mRNA expression in MV-4-11 acute myeloid leukemia cells, with an IC50 of 2.9 nM[1]. BRD4 degrader-3 (Example 1a) binds to the purified BRD4 BD1 and BD2 domains, with IC50 values of 15.5 nM and 12.3 nM, respectively. The IC50 of BRD4 degrader-3 binding to full-length BRD4 is 27.1 nM[1].
References:
[1]. Robert Anthony BLAKE, et al. Tert-butyl (s)-2-(4-(phenyl)-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a] [1,4]diazepin-6-yl) acetate derivatives and related compounds as bromodomain brd4 inhibitors for treating cancer. WO2020055976A1.
In Vitro, BRD4 degrader-3 (6 days) inhibits the proliferation of PC-3-STEAP-1 and EoL-1 cells, with IC50 values of 6.6 nM and 2.2 nM, respectively[1]. BRD4 degrader-3 (4 h) affects MYC mRNA expression in MV-4-11 acute myeloid leukemia cells, with an IC50 of 2.9 nM[1]. BRD4 degrader-3 (Example 1a) binds to the purified BRD4 BD1 and BD2 domains, with IC50 values of 15.5 nM and 12.3 nM, respectively. The IC50 of BRD4 degrader-3 binding to full-length BRD4 is 27.1 nM[1].
References:
[1]. Robert Anthony BLAKE, et al. Tert-butyl (s)-2-(4-(phenyl)-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a] [1,4]diazepin-6-yl) acetate derivatives and related compounds as bromodomain brd4 inhibitors for treating cancer. WO2020055976A1.