PX-12

製品コードS7947 バッチS794702

印刷

化学情報

Chemical Structure Synonyms DB05448, 1-methyl propyl 2-imidazolyl disulfide Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C7H12N2S2
分子量 188.31 CAS No. 141400-58-0
Solubility (25°C)* 体外 DMSO 38 mg/mL (201.79 mM)
Ethanol 38 mg/mL (201.79 mM)
Water 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。

 2.400mg/ml (12.74mM) Taking the 1 mL working solution as an example, add 50 μL of 48 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 PX-12 (DB05448、1-メチルプロピル-2-イミダゾリルジスルフィド) は、Trx-1のCys73を不可逆的にチオアルキル化することにより、強力なチオレドキシン-1 (Trx-1)阻害剤となります。フェーズ2。
in vitro In MCF-7 and HT-29 cells, PX-12 prevents the hypoxia (1% oxygen)-induced increase in HIF-1alpha protein, and decreases HIF-1-trans-activating activity, VEGF formation, and inducible nitric oxide synthase. This compound also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9μM, respectively. It also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. In A549 cells, this chemical inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. In hepatocelluar carcinoma cells, it exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity.
in vivo In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF-7 and HT-29 cells
濃度 ~10 μM
反応時間 72 h
実験の流れ Cell growth is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cells are exposed to a range of concentrations of PX-12 or this compound for 16 h in air or hypoxia (1% oxygen). The cells are then washed with warm drug-free medium and grown in air for the remainder of the 72-h incubation.
動物実験 動物モデル Mice bearing MCF-7 tumor xenografts
投薬量 12 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/12657718/
  • https://pubmed.ncbi.nlm.nih.gov/21069338/
  • https://pubmed.ncbi.nlm.nih.gov/24172913/
  • https://pubmed.ncbi.nlm.nih.gov/26550453/

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：

Chrysophanol-mediated trx-1 activation attenuates renal fibrosis through inhibition of the JNK/Cx43 signaling pathway [ Renal Failure, September 5, 2024, 2398710]
Thioredoxin activity confers resistance against oxidative stress in tumor-infiltrating NK cells [ Journal of Clinical Investigation, October 1, 2020, 5508-5522] PubMed: 32673292
Nuclear translocation of thioredoxin-1 promotes colorectal cancer development via modulation of the IL-6/STAT3 signaling axis through interaction with STAT3 [ Theranostics, August 28, 2023, 4730-4744] PubMed: 37771783
Integrating Differential Gene Expression Analysis with Perturbagen-Response Signatures May Identify Novel Therapies for Thyroid-Associated Orbitopathy [ Translational Vision Science & Technology, August 25, 2020, 39] PubMed: 32908802
Substrate Stiffness Modulates Fibroblast Extracellular Vesicle Secretion via Mechanotransduction Pathways [ bioRxiv, 2025, 2025.07.29.667440] PubMed: 40766685
Nuclear translocation of thioredoxin-1 promotes colorectal cancer development via modulation of the IL-6/STAT3 signaling axis through interaction with STAT3 [ Theranostics, 2023, 13(14):4730-4744] PubMed: 37771783
The cold-inducible RNA-binding protein-Thioredoxin 1 pathway ameliorates mitochondrial dysfunction and mitochondrial dynamin-related protein 1 level in the hippocampus of aged mice with perioperative neurocognitive dysfunction [ CNS Neurosci Ther, 2023, 10.1111/cns.14433] PubMed: 37641878
Ferroptosis heterogeneity in triple-negative breast cancer reveals an innovative immunotherapy combination strategy [ Cell Metab, 2022, S1550-4131-2200411-9] PubMed: 36257316
TXN inhibitor impedes radioresistance of colorectal cancer cells with decreased ALDH1L2 expression via TXN/NF-κB signaling pathway [ Br J Cancer, 2022, 10.1038/s41416-022-01835-1] PubMed: 35597868
Thioredoxin-1 inhibits amyloid-β25-35-induced activation of NLRP1/caspase-1/GSDMD pyroptotic pathway in PC12 cells [ Mol Biol Rep, 2022, 10.1007/s11033-022-07177-8] PubMed: 35072836

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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