KI-TOX-A3 is a TOX protein-protein interaction inhibitor that blocks the TOX-KAT7 protein-protein interaction with an IC 50 of 0.51 μM. KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reverses exhaustion of CD8 + T cells, and inhibits the proliferation of T cell acute lymphoblastic leukemia (T-ALL) cells. KI-TOX-A3 shows promise for use in studies of hematological malignancies such as T-ALL.
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