Aprotinin (Traskolan) is a broad-spectrum serine protease (BPTI) inhibitor that inhibits the activity of a number of different esterases and proteases. Aprotinin is an antifibrinolytic agent used to minimize hemorrhage during complex surgical procedures.

Chymotrypsin:9.5 nM(Kd), Kallikrein:0.8 nM(Kd), Trypsinogen:2 μM(Kd), Trypsin:0.06 pM(Kd)

METHODS: Hepatocellular carcinoma cell lines Hep3B and HCCLM3 were treated with Cepharanthine (1-100 µM) for 48 h and cell viability was measured by CCK-8 assay.
RESULTS: Cepharanthine treatment for 48 h significantly inhibited the viability of Hep3B and HCCLM3 cell lines in a dose-dependent manner at a value of approximately 20 µM. [1]
METHODS: The human hepatocellular carcinoma cell line HuH-7 was treated with Cepharanthine (20 µM) for 7.5-240 min, and the expression levels of target proteins were detected by Western Blot.
RESULTS: Cepharanthine induced time-dependent phosphorylation of JNK and p38 MAPK. c-Jun (Ser 73) and ATF-2, downstream targets of JNK and p38, were significantly activated by Cepharanthine. Cepharanthine caused significant activation of ERK1/2, while Akt was down-regulated by Cepharanthine. [2]

METHODS: To detect anti-tumor activity in vivo, Cepharanthine (10-20 mg/kg) was injected intraperitoneally into nude mice bearing Hep3B xenografts every two days for 24 days.
RESULTS: Cepharanthine treatment significantly prolonged the survival time of nude mice with transplanted tumors. Cepharanthine treatment significantly inhibited the growth of transplanted tumors in vivo. [1]

Substrates and kinases are diluted in 50?mM Tris/HCl (pH?7.5), 0.1% 2-mercaptoethanol, 0.1?mM EGTA and 10?mM magnesium acetate. Reactions are initiated with [γ-32P]ATP (2500 c.p.m./pmol) to a final concentration of 0.1?mM and terminated after 15?min at 30°C by the addition of SDS and EDTA (pH?7.0) to final concentrations of 1.0% (w/v) and 20?mM respectively. After heating for 5?min at 100°C and separation by SDS/PAGE, the phosphorylated proteins are detected by autoradiography.

Mouse G8-1 myoblasts are plated DMEM + 20% FBS (maintenance medium), in which they remain undifferentiated. When cells reach approximately 40-50% confluence, different protease inhibitors are added to the culture media and cells are incubated overnight. Cells are then switched to differentiation-promoting media (DMEM + 10% horse serum ± protease inhibitor) and incubated for 7 days. (Only for Reference)