RK-33

製品コードS8246 バッチS824603

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H20N6O3
分子量 428.44 CAS No. 1070773-09-9
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MDA-MB-231 cells
濃度 7.5 μM
反応時間 12 h
実験の流れ

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.
動物実験 動物モデル SCID mice
投薬量 20 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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