RK-33

製品コードS8246 バッチS824601

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 40 mg/mL (93.36 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

2.000mg/ml (4.67mM) Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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. This compound inhibits cancer growth and radiosensitizes lung cancer cells in a DDX3-dependent manner. It has no effect on either mitochondrial respiration or ATP generation. This chemical curbs proliferation and induces apoptosis in a DDX3-dependent fashion. Wnt signaling is mediated by DDX3 and inhibited by RK-33. It 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. This compound, at the dose used, is non-toxic in SCID mice. This chemical-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 this compound (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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/25820276/

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:

G3BP-driven RNP granules promote inhibitory RNA-RNA interactions resolved by DDX3X to regulate mRNA translatability [ Mol Cell, 2025, 85(3):585-601.e11] PubMed: 39729994
Proliferating Microglia Exhibit Unique Transcriptional and Functional Alterations in Alzheimer's Disease [ ASN Neuro, 2025, 17(1):2506406] PubMed: 40387894
RNA helicase DDX3X promotes NK cell survival by supporting MCL1 expression [ J Immunol, 2025, vkaf281] PubMed: 41100195
DDX3X/MAVS alleviates doxorubicin‑induced cardiotoxicity by regulating stress granules [ Mol Med Rep, 2025, 32(3)237] PubMed: 40576139
DDX3 participates in miRNA biogenesis and RNA interference through translational control of PACT and interaction with AGO2 [ FEBS Open Bio, 2025, 15(1):180-195] PubMed: 39543456
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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。