RK-33

RK-33 (1070773-09-9) is an inhibitor of the RNA helicase DDX3 – IC50’s = 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 References/Citations: 1) Kondaskar et al. (2011), Novel, Broad Spectrum Anticancer Agents Containing the Tricyclic 5:7:5-Fused Diimidazodiazepine Ring System; ACS Med. Chem. Lett., 2 2522) Bol et al. (2015), Targeting DDX3 with a small molecule inhibitor for lung cancer therapy; EMBO Mol. Med., 7 6483) Heerma van Voss et a