Herboxidiene

Herboxidiene is described as a polyketide microbial product, originated from Streptomyces chromofuscus, with antitumor activity. Herboxidiene seems to serve as a novel splicing inhibitor that specifically impairs the SF3b function by binding to SAP155. Herboxidiene in house activity data obtained from our manufacturing partner: Cellular line A549 (lung cancer) IC50: 0,036 ug/ml - IC50 82 uM; Cellular line H116 (colon cancer) IC50 0,01 µg/ml - IC50 22,7 µM; Cellular line PSN1 (pancreatic cancer) IC50 0,036 µg/ml - IC50 82 µM - Cellular line T98G (glioblastoma) IC50 1 µg/ml - IC50 20,5 nM. The splicin modulator also reduced the amount of ubiquitin-specific protease USP19-CY in the cell culture, which led to an inhibition of breast cancer cell migration. Furthermore it displays anti-angiogenic activity via down-regulation of VEGFR-2 and HIF-1-ALPHA. Literature/References: Martinez-Montiel et al. (2016), Microbial and Natural Metabolites That Inhibiting Splicing: A Powerful Alternative for Cancer Treatment; biomed. Res. Int., epub ahead of print Bioactivity: phytotoxic, herbicidal, cytotoxic, IC50 0.0037-0.99 mM, antibiotic Compound class: Polyketide. Potential mode of action/Key words: Targeting RNA, Antitumoral