NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5; Black: linker; Blue: VHL E3 ligase ligand ) [1].
In Vivo, NR-11c (15 mg/kg; intra/peritumoral injection; single dose) down-regulates p38α level in tumor for both administration modes in mouse breast cancer models[1].
In Vitro, NR-11c (1-1000 nM; 24 h) effectively degrades p38α in a variety of tumor cell lines, among which in MDA-MB-231 cells, DC50 is 11.55 nM[1].
References:
[1]. Cubillos-Rojas M, et al. Synthesis and Biological Activity of a VHL-Based PROTAC Specific for p38α. Cancers (Basel). 2023 Jan 18;15(3):611.
In Vivo, NR-11c (15 mg/kg; intra/peritumoral injection; single dose) down-regulates p38α level in tumor for both administration modes in mouse breast cancer models[1].
In Vitro, NR-11c (1-1000 nM; 24 h) effectively degrades p38α in a variety of tumor cell lines, among which in MDA-MB-231 cells, DC50 is 11.55 nM[1].
References:
[1]. Cubillos-Rojas M, et al. Synthesis and Biological Activity of a VHL-Based PROTAC Specific for p38α. Cancers (Basel). 2023 Jan 18;15(3):611.