
SPA-10091-HCl is a degrader of DOT1L that selectively degrades DOT1L protein through the nuclear ubiquitin-proteasome pathway, thereby suppressing H3K79 methylation in CRPC cells. It also inhibits DOT1L enzymatic activity with an IC50 of 0.87 μM, induces apoptosis, and significantly reduces tumor growth in vivo.
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