THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer.
THK01 (1.25-10 μM; 48 h) suppresses the migration and invasion abilities of MDA-MB-231 cells in a dose-dependent manner[1].THK01 (5 μM; 24 h; MDA-MB-231 cells) suppresses breast cancer metastasis through STAT signal pathway[1].THK01 (1.25-10 μM; 24 h; MDA-MB-231 cells) down-regulates the phosphorylation level of STAT3Y705 in a dose-dependent manner, while slightly up-regulates the level of STAT3S727[1].
THK01 (15 mg/kg; i.v.; Female BALB/c nude mice) suppresses cell metastasis of breast cancer in vivo[1].
References:
[1]. Wang J, et, al. Discovery of unglycosylated indolocarbazoles as ROCK2 isoform-selective inhibitors for the treatment of breast cancer metastasis. Eur J Med Chem. 2023 Mar 15;250:115181.