
簡要描述:PX-12 141400-58-0PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1(Trx-1) currently in clinical development as an antitumor agent; IC50=7 uM in Hela, MTT assay, 72 h.
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| 品牌 | absin | CAS | 141400-58-0 |
|---|---|---|---|
| 分子式 | C7H12N2S2 | 純度 | 98% |
| 分子量 | 188.32 | 貨號 | abs47027977 |
| 規(guī)格 | 5mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is an irreversible inhibitor of Thioredo | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
PX-12 141400-58-0
| 產(chǎn)品描述 | |
| 描述 | PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1(Trx-1) currently in clinical development as an antitumor agent; IC50=7 uM in Hela, MTT assay, 72 h. |
| 純度 | 98% |
| 儲存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | PX12; PX 12; IV-2 |
| 外觀 | 類白色至褐色固體 |
| 可溶性/溶解性 | DMSO : 18.8 mg/mL (100 mM); Ethanol : 38 mg/mL (201.79 mM) |
| 生物活性 | |
| 靶點(diǎn) | Trx-1 |
| In vitro(體外研究) | 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 2.9μM, respectively. PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity. |
| In vivo(體內(nèi)研究) | In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density. |
| 參考文獻(xiàn) | |
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| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Signal TransductionMetabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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