O O O O OH OH H

Herboxidiene

Article number:

5500650

CAS No.:

142861-00-5

Formula:

C25H42O6

Chemical description:

2-[(2R,5S,6S)-6-[(2E,4E,6S)-7-[(2R,3R)-3-[(2R,3R,4R)-4-hydroxy-3-methoxypentan-2-yl]-2-methyloxiran-2-yl]-6-methylhepta-2,4-dien-2-yl]-5-methyloxan-2-yl]acetic acid

Synonyms:

GEX-1A; 2H-Pyran-2-acetic acid, tetrahydro-6-(6-(3-(3-hydroxy-2-methoxy-1-methylbutyl)-2-methyloxiranyl)-1,5-dimethyl-1,3-hexadienyl)-5-methyl-; 2,3-anhydro-2-{(2S,3E,5E)-6-[(2S,3S,6R)-6-(carboxymethyl)-3-methyltetrahydro-2H-pyran-2-yl]-2-methylhepta

Molecular weight:

438,30 g/mol

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

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Herboxidiene

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