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PX 12
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PX 12图片
CAS NO:141400-58-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
PX 12(IV-2) 是硫氧还蛋白-1 (Trx-1) 的不可逆抑制剂;抑制 MCF-7 和 HT-29 细胞的生长,IC50 值分别为 1.9 和 2.9 μM。
Cas No.141400-58-0
别名2-(仲丁基二硫基)-1H-咪唑,IV-2
化学名2-(butan-2-yldisulfanyl)-1H-imidazole
Canonical SMILESCCC(C)SSC1=NC=CN1
分子式C7H12N2S2
分子量188.31
溶解度≥ 8.75mg/mL in DMSO, ≥ 99 mg/mL in EtOH
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PX 12 is an inhibitor of thioredoxin-1 [1].

Thioredoxin-1 (Trx-1) is a small redox protein with a conserved catalytic site and plays an important role in cells that includes the regulation of trans-activating activity and the DNA binding of redox-sensitive transcription factors [1].

In HT-29 human colon carcinoma cells and MCF-7 human breast cancer, PX 12 prevented the hypoxia-induced increase in HIF-1 protein. Also, PX 12 decreased inducible nitric oxide synthase, HIF-1-trans-activating activity and VEGF formation [2].

In immunodeficient mice bearing HT-29 human colon xenografts, PX 12 decreased the average tumor blood vessel permeability by 63% within 2 hours and returned to pretreatment values after 48 hours. PX 12 reduced tumor-derived VEGF and tumor after 24 hours. Also, Trx-1 showed a rapid decrease within 2 hours and maintained for 24 hours [1]. In mice bearing MCF-7 tumor xenografts, PX 12 reduced HIF-1ɑ and VEGF protein levels [2]. In cancer patients, PX-12 treatment significantly reduced the levels of Trx-1 and VEGF in plasma [3].

References:
[1].  Jordan BF, Runquist M, Raghunand N, et al. The thioredoxin-1 inhibitor 1-methylpropyl 2-imidazolyl disulfide (PX-12) decreases vascular permeability in tumor xenografts monitored by dynamic contrast enhanced magnetic resonance imaging. Clin Cancer Res, 2005, 11(2 Pt 1): 529-536.
[2].  Welsh SJ, Williams RR, Birmingham A, et al. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1alpha and vascular endothelial growth factor formation. Mol Cancer Ther, 2003, 2(3): 235-243.
[3].  Baker AF, Dragovich T, Tate WR, et al. The antitumor thioredoxin-1 inhibitor PX-12 (1-methylpropyl 2-imidazolyl disulfide) decreases thioredoxin-1 and VEGF levels in cancer patient plasma. J Lab Clin Med, 2006, 147(2): 83-90.