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RK-33

Cat. No. M10506
RK-33 Structure
Synonym:

RK33

Size Price Availability Quantity
2mg USD 80  USD80 In stock
5mg USD 140  USD140 In stock
10mg USD 256  USD256 In stock
25mg USD 442  USD442 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 428.44
Formula C23H20N6O3
CAS Number 1070773-09-9
Purity >99%
Solubility DMSO 30 mg/mL
Storage at -20°C
References

[1] Min Xie, et al. Cancer Res. RK-33 Radiosensitizes Prostate Cancer Cells by Blocking the RNA Helicase DDX3

[2] Guus Martinus Bol, et al. Cancer Chemother Pharmacol. PLGA nanoparticle formulation of RK-33: an RNA helicase inhibitor against DDX3

[3] Guus M Bol, et al. EMBO Mol Med. Targeting DDX3 with a small molecule inhibitor for lung cancer therapy

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RK-33, RK33 supplier, DNA/RNA Synthesis, inhibitors

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