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  3. RK-33

RK-33 is an RNA helicase inhibitor against DDX3, and inhibits its helicase activity.

For research use only. We do not sell to patients.

CAS No. : 1070773-09-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of RK-33:

Top Publications Citing Use of Products

    RK-33 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 May:232:330-339.  [Abstract]

    RK-33 (5 μM; 24 h), a DDX3-specific inhibitor, reinforced increased lipid peroxidation levels in BT549 cells in the presence of hydrogen peroxide.

    RK-33 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 May:232:330-339.  [Abstract]

    RK-33 (5 μM; 24 h) elevated the levels of lipid peroxidation in MCF7/DDX3X-HA cells when they were exposed to hydrogen peroxide.

    RK-33 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 May:232:330-339.  [Abstract]

    RK-33 (5-10 μM; 24 h) dose-dependently suppressed GPX4 protein levels in BT549 and MCF7 cells.

    RK-33 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Apr:117:109779.  [Abstract]

    RK-33 (20 mg/kg; i.p.; once daily) down-regulated the levels of CRP, IL-6 and TNF-α in the peripheral blood of CLP-induced septic mice.

    RK-33 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Apr:117:109779.  [Abstract]

    RK-33 (20 mg/kg; i.p.; once daily) improved the total number of CD4+ and CD8+ T cells in septic mice reduced by CLP.

    View All DNA/RNA Synthesis Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    RK-33 is an RNA helicase inhibitor against DDX3, and inhibits its helicase activity.

    IC50 & Target

    Helicase

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    2.5 μM
    Compound: 1
    Cytotoxicity against human A549 cells after 72 hrs by WST1 assay
    Cytotoxicity against human A549 cells after 72 hrs by WST1 assay
    [PMID: 21572541]
    A549 IC50
    2.56 μM
    Compound: 1
    Cytotoxicity against human A549 cells after 72 hrs by WST1 assay
    Cytotoxicity against human A549 cells after 72 hrs by WST1 assay
    [PMID: 23290252]
    Daoy IC50
    2.5 μM
    Compound: RK-33
    Antiproliferative activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
    Antiproliferative activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTS assay
    [PMID: 33636537]
    Huh-7 CC50
    < 10 μM
    Compound: 51
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability
    Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability
    [PMID: 35899912]
    MCF7 IC50
    7.5 μM
    Compound: 1
    Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay
    Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay
    [PMID: 21572541]
    MCF7 IC50
    7.59 μM
    Compound: 1
    Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay
    Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay
    [PMID: 23290252]
    MDA-MB-231 IC50
    4.01 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by WST1 assay
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by WST1 assay
    [PMID: 21572541]
    MDA-MB-231 IC50
    4.05 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by WST1 assay
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by WST1 assay
    [PMID: 23290252]
    NCI-H460 IC50
    2.8 μM
    Compound: 1
    Cytotoxicity against human H460 cells after 72 hrs by WST1 assay
    Cytotoxicity against human H460 cells after 72 hrs by WST1 assay
    [PMID: 21572541]
    NCI-H460 IC50
    2.87 μM
    Compound: 1
    Cytotoxicity against human H460 cells after 72 hrs by WST1 assay
    Cytotoxicity against human H460 cells after 72 hrs by WST1 assay
    [PMID: 23290252]
    OVCAR-3 IC50
    14.5 μM
    Compound: 1
    Cytotoxicity against human OVCAR3 cells after 72 hrs by WST1 assay
    Cytotoxicity against human OVCAR3 cells after 72 hrs by WST1 assay
    [PMID: 21572541]
    OVCAR-3 IC50
    14.5 μM
    Compound: 1
    Cytotoxicity against human OVCAR3 cells after 72 hrs by WST1 assay
    Cytotoxicity against human OVCAR3 cells after 72 hrs by WST1 assay
    [PMID: 23290252]
    PC-3 IC50
    4.8 μM
    Compound: 1
    Cytotoxicity against human PC3 cells after 72 hrs by WST1 assay
    Cytotoxicity against human PC3 cells after 72 hrs by WST1 assay
    [PMID: 21572541]
    PC-3 IC50
    4.9 μM
    Compound: 1
    Cytotoxicity against human PC3 cells after 72 hrs by WST1 assay
    Cytotoxicity against human PC3 cells after 72 hrs by WST1 assay
    [PMID: 23290252]
    Vero CC50
    29.7 μM
    Compound: 51
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 22 hrs by XTT assay
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 22 hrs by XTT assay
    [PMID: 35899912]
    Vero C1008 CC50
    > 30 μM
    Compound: 51
    Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability
    Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability
    [PMID: 35899912]
    In Vitro

    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[1]. 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[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    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[1]. 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[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    428.44

    Formula

    C23H20N6O3

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1N(CC2=CC=C(OC)C=C2)C3=NC=NC4=C(N=CN4CC5=CC=C(OC)C=C5)C3=N1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (58.35 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3340 mL 11.6702 mL 23.3405 mL
    5 mM 0.4668 mL 2.3340 mL 4.6681 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 2 mg/mL (4.67 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation
    References
    Cell Assay
    [2]

    Briefly, 8×102 MCF-7 cells are seeded in a 96-well plate, and treated with different concentrations of RK-33 loaded nanoparticles and unloaded nanoparticles next day. After 72-h incubation, MTS reagent is added to the cells, and the absorbance is measured at 490 nm after 2-h incubation with MTS reagent. The experiment is repeated three independent times.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice are randomLy redistributed into four groups of eight according to their tumor growth, which results in an approximately equal distribution of tumor size at the beginning of radiation and RK-33 drug treatment. The four groups of mice are blindly chosen for four different experimental procedures, including control (injection of DMSO only), RK-33 treatment (injection of RK-33 only 50 mg/kg), radiation (one-time radiation of 5 Gy), or radiation and RK-33 treatment (combination of radiation of 5 Gy and RK-33 injection). RK-33 and DMSO are injected intraperitoneally thrice weekly for two weeks. Radiation is performed at the beginning of drug injection using the Small Animal Radiation Research Platform (SARRP) with a circular beam of 1 cm diameter, focusing on the tumor site. Mice of each group are euthanized 0 h and 24 h after radiation and tumors are extracted for γH2AX, cleaved Caspase 3, and Ki67 staining. The remaining mice of each group are imaged with a Xenogen IVIS Spectrum, with injection of D-luciferin 5 minutes before imaging. Mice are euthanized after six weeks of imaging and tumors are extracted for H&E staining, cleaved Caspase 3, and i67 staining. Morphology of the tumors after RK-33 and radiation treatment is assessed by a veterinary pathologist on hematoxylin and eosin stained sections.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3340 mL 11.6702 mL 23.3405 mL 58.3512 mL
    5 mM 0.4668 mL 2.3340 mL 4.6681 mL 11.6702 mL
    10 mM 0.2334 mL 1.1670 mL 2.3340 mL 5.8351 mL
    15 mM 0.1556 mL 0.7780 mL 1.5560 mL 3.8901 mL
    20 mM 0.1167 mL 0.5835 mL 1.1670 mL 2.9176 mL
    25 mM 0.0934 mL 0.4668 mL 0.9336 mL 2.3340 mL
    30 mM 0.0778 mL 0.3890 mL 0.7780 mL 1.9450 mL
    40 mM 0.0584 mL 0.2918 mL 0.5835 mL 1.4588 mL
    50 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1670 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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    Cat. No.:
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