SJ3149

Biological Activity

SJ3149 is a uniquely potent and selective CK1α degrader with DC50 of 3.7 nM. SJ3149 shows high activity across a range of acute leukemia (AL) cell lines derived from different hematologic neoplasms, such as B-cell and T-cell acute lymphoblastic leukemia. SJ3149 activity shows a strong correlation with wild-type TP53 expression.SJ3149 (SJ-3149) is uniquely potent and selective CK1α degrader with DC50 of 3.7 nM and Dmax 95% in MOLM-13 cells, potently inhibits the viability of MOLM-13 cells with IC50 of 13 nM. SJ 3149 shows a broad antiproliferative profile on a panel of AML and ALL cell lines with IC50 values in a single digit nanomolar range, and even sub-nanomolar activity. SJ-3149 also potently inhibited the viability of multiple cell lines derived from solid tumors, including breast, soft tissue, and tumors of the male and female reproductive system, with several cell lines being inhibited more potently than MOLM-13. SJ3149 also inhibits several TP53-altered cell lines, such as BT-20 and KU812.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.