PX-12

製品コードS7947 バッチS794701

印刷

化学情報

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 1 30%PEG300 2 65%ddH2O 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。	1.200mg/ml (6.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 650 μL of ddH2O to adjust the volume to 1 mL. 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/

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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]
Chrysophanol-mediated trx-1 activation attenuates renal fibrosis through inhibition of the JNK/Cx43 signaling pathway [ Renal Failure, September 05 2024, 2398551]	PubMed: 39238246
Thioredoxin activity confers resistance against oxidative stress in tumor-infiltrating NK cells [ Journal of Clinical Investigation, October 1, 2020, 5508-5522]	PubMed: 32673292
SLC7A11 Is a Superior Determinant of APR-246 (Eprenetapopt) Response than TP53 Mutation Status [ Molecular Cancer Therapeutics, October 01 2021, 1858-1867]	PubMed: 34315763
Bakuchiol Attenuates Oxidative Stress and Neuron Damage by Regulating Trx1/TXNIP and the Phosphorylation of AMPK After Subarachnoid Hemorrhage in Mice [ Frontiers in Pharmacology, May 15 2020, 712]	PubMed: 32499702
FOXO1 Overexpression Attenuates Tubulointerstitial Fibrosis and Apoptosis in Diabetic Kidneys by Ameliorating Oxidative Stress [ Oxidative Medicine and Cellular Longevity, January 09 2019, 7806046]
Hypoxic Reprogramming of ACOX1-Driven HSP90AB1 Crotonylation Stabilizes Thioredoxin to Orchestrate Redox Homeostasis in Oral Squamous Cell Carcinoma [ Research, February 10 2026, 1129]	PubMed: 41675575
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

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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