RK-33 is a first-in-class, potent and selective DDX3 (RNA helicase) inhibitor, it binds to DDX3 and abrogates its activity. RK-33 caused G1 cell cycle arrest, induced apoptosis, and promoted radiation sensitization in DDX3-overexpressing cells. Inhibition of DDX3 by RK-33 also 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.
Cell Experiment | |
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Cell lines | MDA-MB-231 cells |
Preparation method | Healthy, 60-70% confluent MDA-MB-231 cells are transduced with shDDX3 lentivirus particles. Knockdown of DDX3 expression is confirmed both by qRT-PCR and immunoblotting. MDA-MB-231 cells are treated with RK-33 (7.5 μM) for 12 h and harvested for RNA. Microarray experiments are performed. |
Concentrations | 7.5 μM |
Incubation time | 12 h |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Molecular Weight | 428.44 |
Formula | C23H20N6O3 |
CAS Number | 1070773-09-9 |
Purity | >99% |
Solubility | DMSO 30 mg/mL |
Storage | at -20°C |
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