PROTAC BRD9-binding moiety 5

PROTAC BRD9-binding moiety 5 is a selective BRD9 binder with an IC50 value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

BRD9:4.2 μM (IC50)

PROTAC BRD9-binding moiety 5 (compound 7) (0-250 μM; 48h) has antiproliferative activity against Jurkat, MDA-MB-231, A375 and HCT-116[1]. Cell Proliferation Assay[1] Cell Line: Jurkat, MDA-MB-231, A375 and HCT-116 Concentration: 0-250 μM Incubation Time: 48h Result: Exhibited antiproliferative activity against Jurkat, MDA-MB-231, A375 and HCT-116 with IC50s of 77 ± 7 μM, 125 ± 8 μM, 133 ± 5 μM and 145 ± 3 μM.

[1]. Pierri M, et al. Introducing structure-based three-dimensional pharmacophore models for accelerating the discovery of selective BRD9 binders. Bioorg Chem. 2022 Jan;118:105480.