Hepatocellular carcinoma is the world’s most common primary malignant tumor of the liver. In-Jin-ho-Tang (IJHT) has been used as a traditional Chinese herbal medicine since ancient times,and today it is widely used as a medication for jaundice associated with inflammation of the liver.In-Jin-Ho-Tang is a drug preparation consisting of three herbs: Artemisiae Capillaris Herba(Artemisia capillaries THUNS, Injinho in Korean), Gardeniae Fructus (Gardenia jasminodes ELLIS, Chijain Korean) and Rhei radix et rhizoma (Rheum palmatum L., Daehwang in Korean). This studyinvestigated whether or not methanol extract of IJHT could induce HepG2 cancer cell death.Cytotoxic activity of IJHT on HepG2 cells was measured using an XTT assay, with an IC50 value of700 μg/ml at 24 h Apoptosis induction by IJHT in HepG2 cells was verified by the cleavage ofpoly ADP-ribose polymerase, and a decrease in procaspase-3, -8, -9. Treatment of IJHT resulted inthe release of cytochrome c into cytosol, loss of mitochondrial membrane potential (ΔΨm),decrease in anti-apoptotic Bcl-2, and an increase in pro-apoptotic Bax expression. Thus, IJHTinduced apoptosis in HepG2 cells via activation of caspase and mitochondria pathway. Theseresults indicate that IJHT has potential as an anti-cancer agent.