ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both celllines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).ERD-308 is a highly potent PROTAC degrade
PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 celllines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].
CAY10701 is a 7-deazahypoxanthine analog that prevents microtubule formation, blocking the proliferation of HeLa and MCF-7 cells (GI50s = 22 and 38 nM, respectively). It also inhibits the growth of several different colorectal cancer celllines (GI50 values range from 9 to 17 nM), while being at least 1,500-fold less effective against normal human fibroblast WI38 cells. CAY10701 is effective in vivo, reducing tumor volume in colorectal cell xenografts in mice without significantly altering body weight.
CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 celllines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.