Diazepinomicin

Diazepinomicin (ECO-4601) is an anticancer and antibacterial agent. Diazepinomicin can be produced by a Micromonospora strain. Diazepinomicin induces Apoptosis. Diazepinomicin inhibits the proteases Rhodesain and Cathepsin L at an IC₅₀ of 70-90 μM. Diazepinomicin possesses anti-inflammatory and anti-tumor activity. Diazepinomicin has demonstrated activity against hepatocellular carcinoma. Diazepinomicin shows antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC₅₀ of 13.5 μM. Diazepinomicin exhibits moderate antibacterial activity against specific Gram-positive bacteria, with an MIC of approximately 32 μg/mL^[1][2]. IC50 & Target:Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway post Ras prenylation and prior to MEK activation^[1]. In Vitro:Diazepinomicin (1-25 μM; 24-72 h) induces dose-dependent antiproliferative activity in hepatocellular carcinoma HepG2 cells^[1].
Diazepinomicin exhibits moderate antibacterial activity against specific Gram-positive bacteria, with an MIC of approximately 32 μg/mL^[2].