Cysmethynil

Cysmethynil is an Icmt inhibitor(IC₅₀ = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research^[1][2][3]. IC50 & Target:IC₅₀ = 2.4 μM for Icmt In Vitro:Cysmethynil (15 μM or 20 μM or 30 μM; 6 days) inhibits Icmt^+/+ cells and Icmt^-/-/ICMT cells proliferation, unaffects Icmt^-/-cells growth ^[1].
Cysmethynil (20-30 μM; 1-6 days) inhibits PC3 cells proliferation and results in a dose- and time-dependent reduction in the number of viable PC3 cells^[2].
In Vivo:Cysmethynil (100 mg/kg, 200 mg/kg; intraperitoneal injection; every 48 h; 28 day) without adverse effects on mice body weight, significantly impacts on tumor growth, causes both an accumulation of cells in the G1 phase and cell death ^[2].
Cysmethynil (20 mg/kg; intraperitoneal injection; three times a week; 2 weeks; alone or combined with Paclitaxel  (HY-B0015)/ Doxorubicin (HY-15142A) ) is not toxic to mice and induces only moderate inhibition of tumor growth as single agent, the combination with Paclitaxel(HY-B0015)/ Doxorubicin(HY-15142A) results in significantly greater efficacy in inhibiting tumor growth. Cysmethynil sensitizes cervical cancer cells to chemotherapy agent in xenograft mouse model^[3].