RK-33

Research use only, not for human use.

RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.

RK-33 is a potent and selective DDX3 inhibitor. RK-33 binds to DDX3 and abrogates its activity. Inhibition of DDX3 by RK-33 caused G1 cell cycle arrest, induced apoptosis, and promoted radiation sensitization in DDX3-overexpressing cells. Overall, inhibition of DDX3 by RK-33 promotes tumor regression, thus providing a compelling argument to develop DDX3 inhibitors for lung cancer therapy. RK-33 radiosensitizes prostate cancer cells by blocking the RNA helicase DDX3.

RK-33 shows inhibition of many kinds of cancer cells with IC50 of 3-6 μM, while PC3 is much less sensitive to RK-33 (IC50 >12 μM). RK-33 treatment causes a significant accumulation in the G1 phase for DU145 and LNCaP, although treatment with RK-33 causes only a moderate accumulation of the G1 phase for 22Rv1, and the treated cells have significantly reduced G2 phase. RK-33 treatment also causes 12 moderate G1 accumulation in 22Rv1. RK-33-loaded NPs demonstrate cytotoxicity to MCF-7 cells in a dose-dependent manner, while equivalent doses of empty NPs have no killing effect. The IC50 value of 5% RK-33 loaded NPs is 49 μg/mL, and the IC50 value of 10% RK-33 loaded NPs is 25 μg/mL.

There is more cell death (pyknotic or condensed nuclei) admixed with fibrin and interstitial edema in the tumors from mice from the combination RK-33 and radiation group compared to the control or single treatment groups. The treatment combination of RK-33 and radiation has an advantage in reducing tumor proliferation. In the mice treated with RK-33-PLGA, RK-33 can be detected in the plasma (34 μg/mL) and liver (28 μg/g), but not lungs.

RK-33 | RK 33 | RK33.

Others

Other Targets

DDX3

Cancer

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1070773-09-9

428.44

C23H20N6O3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (116.70 mM)

COC1=CC=C(C=C1)CN2C=NC3=C2N=CN=C4C3=NC(=O)N4CC5=CC=C(C=C5)OC

3,7-dihydro-3,7-bis[(4-methoxyphenyl)methyl]-2H-diimidazo[4,5-d:4',5'-f][1,3]diazepin-2-one

(-20℃)

With Ice Pack

≥ 2 years