Cl-OCH3

Cl-OCH3 is an antagonist of nuclear receptor NR4A1, decreases PD-L1 protein expression in MDA-MB-231 and 4T1 cells with EC50 of 4.4 and 4.1 uM, respectively;Cl-OCH3 decreased expression of PD-L1 mRNA, promoter-dependent luciferase activity, and protein.In in vivo studies using a syngeneic mouse model bearing orthotopically injected 4T1 cells, Cl-OCH3 decreased tumor growth and weight and inhibited lung metastasis.Cl-OCH3 also decreased expression of CD3+/CD4+/CD25+/FoxP3+ regulatory T cells and increased the Teff/Treg ratio.

1. Keshav Karki, et al. Cancer Res. 2020 Mar 1;80(5):1011-1023.