https://www.selleckchem.com/pr....oducts/debio-0123.ht
To achieve a cure of multiple myeloma (MM), we have been developing novel therapies targeting epigenetic aberrations. EZH2 and its homolog EZH1 are the histone lysine methyltransferases inducing the repressive mark of H3K27me3. UNC1999 is a dual inhibitor of EZH2 and EZH1, showing significant anti-MM activities. It also synergizes with proteasome inhibitors, associated with derepression of NR4A1 and downregulation of MYC. Moreover, UNC1999 and a selective Akt inhibitor TAS-117 synergistically inhibit the growth of MM cells through ep
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