PX-12

别名: DB05448, 1-methyl propyl 2-imidazolyl disulfide

PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide)是一种有效的 thioredoxin-1 (Trx-1) 抑制剂,作用于 Trx-1 上 Cys73 的不可逆硫代烷基化。Phase 2。

PX-12 Chemical Structure

PX-12 Chemical Structure

CAS: 141400-58-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 810.81 现货
10mg RMB 794.43 现货
50mg RMB 3087.63 现货
200mg RMB 7182.63 现货
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产品质控

批次: 纯度: 99.99%
99.99

PX-12相关产品

Thioredoxin抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
M21 Function assay 25 nM 16 hrs Stimulation of nuclear translocation of thioredoxin-1 from cytosol in human M21 cells at 25 nM after 16 hrs by immunocytofluorescence 18617414
Raji Function assay 5 to 10 uM 4 to 24 hrs Induction of Trx mRNA expression in human Raji cells at 5 to 10 uM after 4 to 24 hrs by RT-PCR analysis 22128876
Raji Function assay 10 to 20 uM 4 to 8 hrs Induction of Trx protein expression in human Raji cells at 10 to 20 uM after 4 to 8 hrs by Western blot analysis 22128876
T84 Function assay 3 hrs Inhibition of human recombinant thioredoxin-mediated TG2 activation expressed in T84 cells assessed as blockade of 5-biotinamidopentylamine incorporation after 3 hrs by fluorescence microscopic analysis, IC50=2.11μM 23327656
Ramos Cytotoxicity assay 72 hrs Cytotoxicity against human Ramos cells after 72 hrs by MTT assay, LD50=3.4μM 22128876
PancO2 Cytotoxicity assay 72 hrs Cytotoxicity against mouse PancO2 cells after 72 hrs by crystal violet staining, LD50=3.9μM 22128876
T24 Cytotoxicity assay 72 hrs Cytotoxicity against human T24 cells after 72 hrs by crystal violet staining, LD50=4.6μM 22128876
B78 Cytotoxicity assay 72 hrs Cytotoxicity against mouse B78 cells after 72 hrs by crystal violet staining, LD50=5μM 22128876
CT26 Cytotoxicity assay 72 hrs Cytotoxicity against wild type mouse CT26 cells after 72 hrs by crystal violet staining, LD50=5.2μM 22128876
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by MTT assay, LD50=5.5μM 22128876
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B method, GI50=8.3μM 18617414
M21 Antiproliferative assay 48 hrs Antiproliferative activity against human M21 cells after 48 hrs by sulforhodamine B method, GI50=8.3μM 18617414
Raji Cytotoxicity assay 72 hrs Cytotoxicity against human Raji cells after 72 hrs by MTT assay, LD50=8.8μM 22128876
EMT6 Cytotoxicity assay 72 hrs Cytotoxicity against mouse EMT6 cells after 72 hrs by crystal violet staining, LD50=11.6μM 22128876
HT29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B method, GI50=25μM 18617414
MEF Cytotoxicity assay Cytotoxicity against mouse MEF cells, LD50=2.7μM 22128876
M21 Antiproliferative assay Antiproliferative activity against human M21 cells, GI50=8.3μM 18502639
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, GI50=8.3μM 18502639
HT29 Antiproliferative assay Antiproliferative activity against human HT29 cells, GI50=25μM 18502639
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide)是一种有效的 thioredoxin-1 (Trx-1) 抑制剂,作用于 Trx-1 上 Cys73 的不可逆硫代烷基化。Phase 2。
靶点
Trx-1 [1]
体外研究(In Vitro)
体外研究活性 在MCF-7和HT-29细胞中,PX-12防止低氧(1% 氧气)诱导的HIF-1alpha蛋白增加,并降低HIF-1反式激活活性,VEGF形成,和诱导型一氧化氮合酶。PX-12也会抑制MCF-7和HT-29细胞的生长,IC50s分别为1.9 μM和2.9μM。[1] PX-12也会通过Nrf2/PMF-1介导的增加抑制HIF-1α蛋白质水平。[2]在A549细胞中,PX-12通过G2/M细胞周期阻滞,和Bax-介导的,ROS-依赖性细胞凋亡抑制细胞生长。[3]在肝癌细胞中,PX-12与5-FU发挥协同作用,显著抑制致瘤性。[4]
细胞实验 细胞系 MCF-7 和 HT-29 细胞
浓度 ~10 μM
孵育时间 72 小时
方法 细胞生长使用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐法测量。在空气或低氧(1% 氧气)条件下,细胞在一系列浓度的PX-12或pleurotin中暴露16小时。然后细胞在空气中用温的不含药物的培养基洗涤,再进行后面的72小时培育。
体内研究(In Vivo)
体内研究活性 在负荷MCF-7肿瘤异种移植物的小鼠中,PX-12 (12 mg/kg, i.p.)降低HIF-1α 与 VEGF蛋白质水平和微血管密度。[1]
动物实验 Animal Models 负荷MCF-7肿瘤异种移植物的小鼠
Dosages 12 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00736372 Completed
Metastatic Cancer|Advanced Cancer
Cascadian Therapeutics Inc.|Seagen Inc.
June 2008 Phase 1
NCT00417287 Terminated
Pancreatic Neoplasms
Cascadian Therapeutics Inc.|National Cancer Institute (NCI)|Translational Genomics Research Institute|Seagen Inc.
December 2006 Phase 2

化学信息&溶解度

分子量 188.31 分子式

C7H12N2S2

CAS号 141400-58-0 SDF Download PX-12 SDF
Smiles CCC(C)SSC1=NC=CN1
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 38 mg/mL ( 201.79 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 38 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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