CBLC000 is a potent inhibitor of FACT (facilitates chromatin transcription) complex that activates p53 and suppresses NF-kB without genotoxicity. CBLC000 induces chromatin trapping of FACT both in vitro and in vivo. CBLC000 exhibits brad anticancer activity. CBLC000 analog clinical candidate CBL0137 decreases self-renewal of GBM stem cells (GSC).
Potent inhibitor of FACT complex that activates p53 and suppresses NF-kB without genotoxicity
Effective eradication of cancer requires treatment directed against multiple targets. The p53 and nuclear factor κB (NF-κB) pathways are dysregulated in nearly all tumors, making them attractive targets for therapeutic activation and inhibition, respectively. We have isolated and structurally optimized
The nearly universal recurrence of glioblastoma (GBM) is driven in part by a treatment-resistant subpopulation of GBM stem cells (GSC). To identify improved therapeutic possibilities, we combined the EGFR/HER2 inhibitor lapatinib with a novel small molecule, CBL0137, which inhibits FACT
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