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- 技术资料
- CAS号：
1401223-22-0
- 规格：
1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥202.0 |
|---|---|---|---|
| 规格： | 2mg | 产品价格： | ￥111.0 |
| 规格： | 5mg | 产品价格： | ￥174.0 |
| 规格： | 10mg | 产品价格： | ￥273.0 |
| 规格： | 25mg | 产品价格： | ￥504.0 |
| 规格： | 50mg | 产品价格： | ￥920.0 |
| 规格： | 100mg | 产品价格： | ￥1368.0 |
Product Introduction
Bioactivity
| 名称 | PI-1840 |
| 描述 | PI-1840（IC50 = 27 nM）is a reversible and selective chymotrypsin-like (CT-L) inhibitor, with little proteasome proteolytic effects on trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L). |
| 细胞实验 | Cells are plated in 96-well plates in 100 μL medium and allowed to attach overnight. Cells are then incubated for 120 h with varying concentrations of inhibitors. Media is aspirated and replaced with 100 μL complete media containing 1 mg/ml MTT and incubated for three hours at 37 °C in 5% CO2 humidified incubator. Media is then aspirated and DMSO is added. Cells are incubated for 10 min at room temperature while shaking, and the absorbance is determined at 540 nm using a μQuant spectrophotometric plate reader. The IC50 values are determined using equation under CT-L, T-L, PGPH-L proteolytic activity assays.(Only for Reference) |
| 激酶实验 | CT-L, T-L, PGPH-L proteolytic activity assays: In the high-throughput screen, fluorogenic peptides are used as substrates to assay (at 10 μM) the 50,000 compounds library from ChemBridge for inhibitory activity against the CT-L proteolytic activity of the purified rabbit 20S proteasome. To test for selectivity for CT-L over T-L and PGPH-L the corresponding fluorogenic peptides are used. Briefly, 1 nM of purified 20S rabbit proteasome is incubated with 20 μM Suc-Leu-Leu-Val-Tyr-AMC for the CT-L activity, Bz-Val-Gly-Arg-AMC for the T-L activity, and benzyloxycarbonyl Z-Leu-Leu-Glu-AMC for the PGPH-L activity for 1 h at 37 °C in 100 μL of assay buffer (50 mM Tris-HCl, pH 7.6) with or without compound. After incubation, production of hydrolyzed 7-amido-4-methyl-coumarin (AMC) groups is measured using a WALLAC Victor2 1420 Multilabel Counter with an excitation filter of 355 nm and an emission filter of 460 nm. The amount of AMC released is within the linear range. Bortezomib is used as a positive control for IC50 determinations. To determine proteasome activity in whole cell, extracts (5 μg) from cultured cell lysate is used instead of 20S rabbit proteasome, and followed the same assay mentioned above. |
| 体外活性 | PI-1840在完整的人类MDA-MB-468癌细胞中强效抑制蛋白酶体CT-L活性，其IC50为0.37 μM，并抑制人类MDA-MB-468细胞的增殖/存活。[1] 在完整的癌细胞中，PI-1840抑制CT-L活性，诱导蛋白酶体底物p27、Bax和IκB-α的积累，抑制存活途径和活性，并诱导凋亡。[2] |
| 体内活性 | PI-1840 (150 mg/kg i.p.) 在小鼠中抑制了MDA-MB-231乳腺肿瘤的生长。[2] |
| 存储条件 | 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 : 31 mg/mL (78.59 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.07 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 72 mg/mL (182.52 mM), Sonication is recommended. |
| 关键字 | U2-OS cells | proteasome substrates | Proteasome | poly ADP ribose polymerase | PI-1840 | PI1840 | PARP | Nuclear factor-κB | Nuclear factor-kappaB | NF-κB | MG-63 cells | Inhibitor | inhibit | Chymotrypsin-like proteasome | cell proliferation | cell cycle | Caspase | Bcl-2 Family | Autophagy | Apoptosis | anticancer |
| 相关产品 | Formamide | D-Psicose | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Metronidazole | Hemin | Hydroxychloroquine | Stavudine | Paeonol | Ethyl linoleate |
| 相关库 | Inhibitor Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Aging Compound Library | Highly Selective Inhibitor Library | Epigenetics Compound Library | Immunology/Inflammation Compound Library | Covalent Inhibitor Library | Target-Focused Phenotypic Screening Library | Anti-Prostate Cancer Compound Library |
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相关实验
体系，可与质子结合，故其碱性（PKb=8.8）较吡咯(pKb=13.6)强，也比苯胺（pKb=9.3）强，能与强酸作用生成较稳定的盐。但比氨(pKb=4.75)弱，也比脂肪叔胺（三甲胺的pKb=4.22）弱。原因在于吡啶环上未参与共轭体系的这一对未共用电子对处于sp2杂化轨道上，其s成分较sp3杂化轨道多，受原子核束缚强，因而较难与H+结合。 吡啶与水能以任意比例混溶，同时又能溶解大多数极性及非极性有机化合物，它是一个良好的溶剂。吡啶具有高水溶性的原因，除分子极性外，是由于其氮原子上一对未参与环
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 PI1840【1401223-22-0】
￥111 - 1368
