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- 2026年07月07日
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- CAS号：
1217022-63-3
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥324.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥856.0 |
| 规格： | 5mg | 产品价格： | ￥679.0 |
| 规格： | 10mg | 产品价格： | ￥984.0 |
| 规格： | 25mg | 产品价格： | ￥2024.0 |
| 规格： | 50mg | 产品价格： | ￥3176.0 |
| 规格： | 100mg | 产品价格： | ￥3784.0 |
Product Introduction
Bioactivity
| 名称 | PTC-209 hydrobromide |
| 描述 | PTC-209 hydrobromide (PTC-209 HBr) is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs). |
| 细胞实验 | To determine whether pretreatment with the inhibitor affects tumor cell growth, cells are plated with the inhibitor for 4 d in vitro and plated in limiting doses in vitro without adding further inhibitor. Trypan blue exclusion is used to count viable cells. The in vitro sphere-initiating cell frequency is calculated after inhibitor treatment by evaluating the number of wells containing spheres. For the experiments where LDAs are set up following recovery of PTC-209 treated cells, 6-well plates were seeded with 1E6 cells per well and incubated overnight. Cells are subsequently treated for 4 d in triplicate with either DMSO vehicle or PTC-209 (0.01, 0.1, 1 and 10 μM). Drug treatments are washed off and 4 mL fresh suspension medium added to all wells. To assess cell viability following the 4 d treatment window, cells are trypsinized and counted at 0, 24, 72 and 120 h after removal of the drug. Long-lasting effects of the drug treatment on sphere-forming ability are assessed by plating LDAs (50,000, 10,000, 1,000,100, 10 and 1 cell per well) using the cells obtained 120 h after the 4-d drug treatment.(Only for Reference) |
| 激酶实验 | Untranslated region-mediated luciferase reporter expression: HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control. |
| 体外活性 | PTC-209在人类结直肠癌细胞HCT116和人类纤维肉瘤细胞HT1080中同时抑制UTR介导的报告基因表达和内源性BMI-1表达。PTC-209通过BMI-1依赖的方式减缓结直肠肿瘤细胞生长。此外，PTC-209还通过不可逆的生长抑制作用损害结直肠癌起始细胞(CICs)。[1] |
| 体内活性 | PTC-209（60 mg/kg/天，皮下注射）有效抑制了肿瘤组织中BMI-1的产生，并在带有初级人类结肠癌异种移植物、人类结肠癌细胞系LIM1215或HCT116异种移植物的小鼠中停止了已建立肿瘤的生长。PTC-209还在体内减少了功能性结直肠CICs的频率。[1] |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : <1 mg/mL H2O : <1 mg/mL 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (5.73 mM), Sonication is recommended. DMSO : 93 mg/mL (161.43 mM), Sonication is recommended. |
| 关键字 | tumor | PTC-209 Hydrobromide | PTC209 Hydrobromide | PTC-209 | PTC209 | PTC 209 Hydrobromide | PTC 209 | lung | Inhibitor | inhibit | HEK293T | colon | CICs | cells | cancer-initiating | breast | BMI-1 | BMI1 | Autophagy | anti-myeloma |
| 相关产品 | Guanidine hydrochloride | Naringin | Enzalutamide | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Paeonol |
| 相关库 | Bioactive Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | DNA Damage & Repair Compound Library |
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文献和实验指先天性对特定味物质缺乏品味能力的现象。对人来说，对特殊化合物的味盲是众所周知的，这里对苯硫脲（ PTC）的味盲是具有代表性的例子。这种物质与具有强甜味的乙氧基苯脲（ dulcin）不同之点，仅在于脲基的 S为 O取代，大多数人对其稀溶液可感到强烈的苦味，但有的人却完全感不到苦味，也有的感受者则感到苦以外的味。对 6377名的某一统计例表明，感到有味者（ taster）占 79.7％，无味者（ notaster）占 20.3％，在有味者当中，感苦味者占 65.4％，感酸味者占
性，并将它们与人类的同类物进行了比较。TAS2R38是人类的一种苦味受体，其中一些人有“超级品尝者”变体，使他们对苦味化合物极端敏感，这解释了一些人对西兰花和芽甘蓝的强烈厌恶。与人类的TAS2R38受体相比，cat版本的Tas2r43对一种叫做PTC的关键苦味化合物的敏感性降低了10倍，对另一种苦味化合物PROP完全没有反应。与人类类似，猫的苦味受体也被苦味化合物芦荟苷（在芦荟植物中发现）和变性氨（用来阻止儿童和宠物食用防冻剂等化学物质）激活，但对这些化合物的反应不同。猫受体对芦荟苷的敏感性较低，对地那酮的敏感
结合以产生某种生理效果的物质。细胞外能与受体结合的分子一般称之为配体，包括激素生长因子，细胞因子，神经递质，还有其他各种各样的小分子化合物；信号传导过程：那么当配体特异性的去结合到细胞膜也或者是细胞内的受体，配体和受体结合之后细胞内的一系列蛋白就会依次对下游蛋白的活性进行调节，包括是激活或者是抑制的作用，从而将外界的信号进行逐步的放大，传递， 最终产生一系列综合性的细胞应答上游蛋白对下游蛋白的调节主要是通过 添加或者去除磷酸基团，从而改变下游蛋白的这个空间构象来完成的。2、蛋白激酶（kinase）蛋白
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