Uses
LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM[1].
Biological Activity
C28 is a potent lemur tyrosine kinase 3 (LMTK3) inhibitor (IC50 = 67 nM). Disrupts interaction of LMTK3 and HSP90 leading to degradation of LMTK3. Also inhibits CLK, DYRK1α, IRAK4 and HIPK2 (IC50 values are 5 nM, 6 nM, 41 nM and 48 nM respectively). C28 inhibits growth and increases apoptosis in breast cancer cell lines (IC50 = 6.5-14.77 μM) and reduces growth of tumors in xenograft and transgenic mouse models of breast cancer. Also reduces levels of ERα.
References
[1] Agnarelli A, et al. The Inhibitory Properties of a Novel, Selective LMTK3 Kinase Inhibitor. Int J Mol Sci. 2023 Jan 3;24(1):865. DOI:
10.3390/ijms24010865
