10058-F4 - CAS 403811-55-2
Catalog number: 403811-55-2
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression.
10058-F4; 10058F4; 10058 F4
Canonical SMILES:
1.A high-throughput screening assay for assessing the viability of Cryptococcus neoformans under nutrient starvation conditions.
Dehdashti SJ;Abbott J;Nguyen DT;McKew JC;Williamson PR;Zheng W Anal Bioanal Chem. 2013 Aug;405(21):6823-9. doi: 10.1007/s00216-013-7134-4. Epub 2013 Jun 30.
Cryptococcus neoformans causes an estimated 600,000 AIDS-related deaths annually that occur primarily in resource-limited countries. Fluconazole and amphotericin B are currently available for the treatment of cryptococcal-related infections. However, fluconazole has limited clinical efficacy and amphotericin B requires intravenous infusion and is associated with high renal toxicity. Therefore, there is an unmet need for a new orally administrable anti-cryptococcal drug. We have developed a high-throughput screening assay for the measurement of C. neoformans viability in 1,536-well plate format. The signal-to-basal ratio of the ATP content assay was 21.9 fold with a coefficient of variation and Z' factor of 7.1% and 0.76, respectively. A pilot screen of 1,280 known compounds against the wild-type C. neoformans (strain H99) led to the identification of four active compounds including niclosamide, malonoben, 6-bromoindirubin-3'-oxime, and 5-[(4-ethylphenyl)methylene]-2-thioxo-4-thiazolidinone. These compounds were further tested against nine clinical isolates of C. neoformans, and their fungicidal activities were confirmed. The results demonstrate that this miniaturized C. neoformans assay is advantageous for the high-throughput screening of large compound collections to identify lead compounds for new anti-cryptococcal drug development.
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