Synonyms: MK-8628 | OTX-015 | OTX015
Compound class:
Synthetic organic
Comment: OTX015 inhibits interaction between bromodomain and extra-terminal (BET) family of bromodomain-containing proteins (BRDs) BET domains and acetylated histone 4 (AcH4). It is an orally available novel BRD2/3/4 inhibitor with potent preclinical anti-tumour activity [1,4,6,10,12-13]. OTX015 is an analogue of (+)-JQ1.
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Bioactivity Comments |
To date affinity data for OTX015 is only available from a meeting abstract [8], in which EC50 values for OTX015 binding to BRD2, BRD3, and BRD4 fall within the 10-19nM range. Biological in vitro and in vivo effects have been reported: for example, preclinical findings in B-cell tumor models [3] and in glioblastoma models [1]. |