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PX-12

PX-12 (PX12) 是一种可逆的硫氧还蛋白-1(Trx-1)抑制剂，能够抑制 MCF-7 细胞(IC50:1.9 μM)和HT-29 细胞(IC50:2.9 μM)的生长。

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

PX12|2-[(1-甲基丙基)二硫代]-1H-咪唑|IV-2

验证数据展示

  • CAS No.: 141400-58-0

    PX-12
    CAS#: 141400-58-0

产品信息

PX-12 (1-methylpropyl 2-imidazolyl disulfide) is a small-molecule inhibitor of Trx-1 (thioredoxin-1), stimulates apoptosis, down-regulates HIF-1α and vascular endothelial growth factor (VEGF) and inhibits tumor growth in animal models. Since high levels of Trx-1 have been associated with colorectal, gastric and lung cancers, PX-12 is indicated as a potential cancer treatment in combination with chemotherapy for patients with advanced metastatic cancer. Initial trials correlated doses of Px-12 with increased patient survival.

CAS号 141400-58-0
分子式 C7H12N2S2
主要靶点 Thioredoxin
主要通路 代谢
分子量 188.32
纯度 99.21%， 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
别名 PX12|2-[(1-甲基丙基)二硫代]-1H-咪唑|IV-2

靶点活性

HT-29 cell:2.9 μM|MCF-7 cell:1.9 μM

体内活性

In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density. [1]

体外活性

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. PX-12 also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9 μM, respectively. [1] PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. [2] In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. [3] In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity. [4]

溶解度

DMSO:18.8 mg/mL(100 mM),Ethanol:38 mg/mL (201.79 mM),H2O:<1 mg/mL

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

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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