RK-33

Catalog No.S8246 Batch:S824603

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Technical Data

Formula

C23H20N6O3
Molecular Weight 428.44 CAS No. 1070773-09-9
Solubility (25°C)* In vitro DMSO 43 mg/mL (100.36 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
DDX3 [1]
In vitro RK-33 binds specifically to DDX3, but not to the closely related proteins DDX5 and DDX17. RK-33 inhibits cancer growth and radiosensitizes lung cancer cells in a DDX3-dependent manner. RK-33 has no effect on either mitochondrial respiration or ATP generation. RK-33 curbs proliferation and induces apoptosis in a DDX3-dependent fashion. Wnt signaling is mediated by DDX3 and inhibited by RK-33. RK-33 impairs radiation-induced DNA damage repair by inhibiting NHEJ activity[1].
In vivo RK-33 in combination with radiation induces tumor regression in multiple mouse models of lung cancer. RK-33, at the dose used, is non-toxic in SCID mice. RK-33-treated mice do not exhibit any discernable morphological changes[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MDA-MB-231 cells

  • Concentrations

    7.5 μM

  • Incubation Time

    12 h

  • 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.
Animal Study:

[1]
  • Animal Models

    SCID mice

  • Dosages

    20 mg/kg

  • Administration

    i.p.

Selleck's RK-33 has been cited by 19 publications

DDX3 regulates cancer immune surveillance via 3' UTR-mediated cell-surface expression of PD-L1 [ Cell Rep, 2024, 43(3):113937] PubMed: 38489268
The mRNA-binding protein DDX3 mediates TGF-β1 upregulation of translation and promotes pulmonary fibrosis [ JCI Insight, 2023, 8(7)e167566] PubMed: 36821384
Inhibition of DDX3X ameliorated CD4+ T cells pyroptosis and improves survival in septic mice [ Mol Immunol, 2023, 154:54-60] PubMed: 36603305
Yin Yang 1 promotes aggressive cell growth in high-grade breast cancer by directly transactivating kinectin 1 [ MedComm (2020), 2022, 3(3):e133] PubMed: 35811688
DDX3 acts as a tumor suppressor in colorectal cancer as loss of DDX3 in advanced cancer promotes tumor progression by activating the MAPK pathway [ Int J Biol Sci, 2022, 18(10):3918-3933] PubMed: 35844798
DDX3X alleviates doxorubicin-induced cardiotoxicity by regulating Wnt/β-catenin signaling pathway in an in vitro model [ J Biochem Mol Toxicol, 2022, e23077] PubMed: 35467791
Selective cell death in HIV-1-infected cells by DDX3 inhibitors leads to depletion of the inducible reservoir [ Nat Commun, 2021, 12(1):2475] PubMed: 33931637
Targeting DDX3X Triggers Antitumor Immunity via a dsRNA-Mediated Tumor-Intrinsic Type I Interferon Response [ Cancer Res, 2021, 81(13):3607-3620] PubMed: 33941613
Proteomic analysis identifies the RNA helicase DDX3X as a host target against SARS-CoV-2 infection [ Antiviral Res, 2021, 190:105064] PubMed: 33781803
Ribosomal Protein L13 Participates in Innate Immune Response Induced by Foot-and-Mouth Disease Virus [ Front Immunol, 2021, 12:616402] PubMed: 34093518

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.