**Background**
Liver cancer remains one of the most challenging malignancies to treat, characterized by high recurrence rates and poor overall survival. Among the various signaling pathways driving tumor progression, the Mixed Signal Transducer (MST) family of kinases plays a critical role in regulating cell survival, proliferation, and apoptosis. Specifically, MST3 has emerged as a potential therapeutic target due to its involvement in oncogenic signaling in various cancers. Inhibiting MST3 may provide a strategic approach to suppress tumor growth and induce programmed cell death in malignant hepatocytes. In this context, we will introduce a selective and orally active MST3 inhibitor – MST3-IN-1.
**Definition**
MST3-IN-1 TFA (Compound LD-1) is a selective MST3 inhibitor with an IC50 value of 122.4 nM. According to the MST3-IN-1 description, this compound is designed as a Riluzole-Ciprofloxacin hybrid to achieve high potency and selectivity.
**In Vitro and In Vivo Studies**
The MST3-IN-1 biological activity has been extensively evaluated in liver cancer models. In vitro studies demonstrated that MST3-IN-1 TFA exhibits significant antiproliferative activity against HepG2 cells. Furthermore, MST3-IN-1 in vitro data indicates that the compound effectively induces apoptosis in HepG2 cells and triggers cell cycle arrest specifically at the G2/M transition. Regarding the MST3-IN-1 In Vivo efficacy, the compound was administered to HepG2 xenograft mice, where it significantly suppressed tumor growth. These results suggest that the compound’s oral activity and selectivity make it a promising candidate for further development in MST3-IN-1 Cancer research. In conclusion, MST3-IN-1 is a potent and selective MST3 inhibitor that holds promise as an effective therapeutic agent for the treatment of liver cancer.
Keywords
MST3-IN-1, Hippo (MST), Caspase, Bcl-2 Family, Apoptosis, MST3, cancer, HepG2 cells, Inhibitor, inhibitor, inhibit
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