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PX-12

CAS号

141400-58-0

分子式

C7H12N2S2

主要靶点

Thioredoxin

仅限科研使用

Cat No : CM06641

Print datasheet

Synonyms

Inhibitor|IV 2|IV2|IV-2|PX12|PX-12|PX 12|TRX (HT-29 cells)|TRX (MCF-7)|2-[(1-甲基丙基)二硫代]-1H-咪唑|inhibit

验证数据展示

  • CAS No.: 141400-58-0

    PX-12
    CAS#: 141400-58-0

产品信息

CAS号 141400-58-0
分子式 C7H12N2S2
主要靶点 Thioredoxin
主要通路 代谢
分子量 188.31
纯度 99.6%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Inhibitor|IV 2|IV2|IV-2|PX12|PX-12|PX 12|TRX (HT-29 cells)|TRX (MCF-7)|2-[(1-甲基丙基)二硫代]-1H-咪唑|inhibit

靶点活性

HT29 cells:2.9 μM|MCF-7 cells:1.9 μM

体内活性

在携带MCF-7肿瘤异种移植的小鼠中，PX-12 (12 mg/kg, i.p.) 降低了HIF-1α和VEGF蛋白水平以及微血管密度。[1]

体外活性

在MCF-7和HT-29细胞中，PX-12抑制低氧（1%氧气）诱导的HIF-1alpha蛋白增加，并减少HIF-1转录激活活性、VEGF形成和可诱导性一氧化氮合酶。PX-12还以1.9μM和2.9μM的IC50抑制MCF-7和HT-29细胞的生长。[1] PX-12通过Nrf2/PMF-1介导的增加还能抑制HIF-1α蛋白水平。[2] 在A549细胞中，PX-12通过G2/M期阻滞以及Bax介导和ROS依赖的凋亡抑制细胞生长。[3] 在肝癌细胞中，PX-12与5-FU协同作用明显抑制肿瘤形成。[4]

溶解度

DMSO:18.8 mg/mL (99.84 mM);Ethanol:38 mg/mL (201.79 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

细胞实验

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 pleurotin 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.(Only for Reference)

参考文献

1.Welsh SJ, et al. Mol Cancer Ther. 2003, 2(3), 235-243.
2.Kim YH, et al. Cancer Chemother Pharmacol. 2011, 68(2), 405-413.
3.You BR, et al. Int J Oncol. 2014, 44(1), 301-308.
4.Li GZ, et al. Am J Transl Res. 2015, 7(9), 1528-1540.
5.Metcalfe C, et al. Thioredoxin Inhibitors Attenuate Platelet Function and Thrombus Formation. PLoS One. 2016 Oct 7;11(10):e0163006

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