RK-33 is an inhibitor of the RNA helicase DDX3 - IC50s = 4.4-8.4 µM in high DDX3 expressing lung cancer cell lines A549, H1299, H23, and H460.1,2 Inhibition of DDX3 led to activation of cell death pathways, inhibition of Wnt pathway signaling, and abrogation of non-homologous end-joining (NHEJ) DNA repair. RK-33 was also active in colorectal cancer 3, prostate cancer4, and medulloblastoma cancer5 cell lines. RK-33 caused radiosensitization in breast cancer through inhibition of mitochondrial translation.6 RK-33 facilitates differentiation in human embryonic stem cells (hESC) and decreases pluripotency markers as well as reducing teratoma formation.7
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