SJ3149 is a selective and potent in vitro and in vivo degrader of CK1α protein with broad antiproliferative activity. SJ3149 can be used in cancer research.
SJ3149 (1 nM-10 µM; 4 h) degrades CK1α protein in MOLM-13 cells by 50 % at a concentration of 4 nM, while at a dose of 10 μM, the level of IKZF2 in the cells is only reduced by about 40 %[1]. SJ3149 inhibits the growth of MOLM-13 cells with an IC50 of 14 nM and reduces CK1a abundance with a DC50 value of 11 nM and a Dmax value of 88 %[2].
SJ3149 (50 mg/kg; i.p.; once a day for 2 days or twice a day for 2 days) significantly degrades CK1α protein levels in NSG mice transplanted with MOLM-13 cells[1].
References:
[1]. Nishiguchi G, et al. Selective CK1α degraders exert antiproliferative activity against a broad range of human cancer cell lines. Nat Commun. 2024 Jan 16;15(1):482.
[2]. Rankovic Z, et al. Rationally Designed Potent and Selective CK1α Degraders Exert Antiproliferative Activity Against a Broad Range of Human Cancer Cell Lines[J]. 2023.