PI-1840
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PI-1840是一种有效的和选择性的蛋白酶体抑制剂,对胰凝乳蛋白酶样(CT-L)活性的IC50值为27 nM[1].
26S蛋白酶体由一个19S调节颗粒(RP)和一个20S核心颗粒组成.26S蛋白酶体具有三个主要的催化活性:胰凝乳蛋白酶样(CT-L)\谷氨酰转肽水解肽样(PGPH-L)和胰蛋白酶样(T-L)活性.CT-L活性在降解肿瘤抑制子和凋亡蛋白方面扮演重要角色[1].
PI-1840是一种快速可逆的和非共价的蛋白酶体CT-L抑制剂.PI-1840对CT-L比对PGPH-L和T-L活性具有更高的选择性.在MDA-MB-468人类乳腺癌细胞中,PI-1840可抑制CT-L活性,IC50值为0.37 μM,并可抑制细胞存活和增殖[1].并且,PI-1840对组成型20S蛋白酶体的选择性比对免疫蛋白酶体强121倍,IC50值分别为18和2170 nM.在MDA-MB-468细胞中,PI-1840可引发CT-L底物IκB-α\p27和Bax积累.并且,PI-1840可降低survivin\p-Akt和Ser(P)-6水平,并能通过聚(ADP-核糖)聚合酶剪切和caspase-3活化诱导细胞凋亡[2].
在携带人类乳腺肿瘤的裸鼠中,PI-1840(150 mg/kg/天,i.p.每天)可抑制85%的肿瘤生长[2].
参考文献：
[1]. Ozcan S, Kazi A, Marsilio F, et al. Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors. J Med Chem, 2013, 56(10): 3783-3805.
[2]. Kazi A, Ozcan S, Tecleab A, et al. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem, 2014, 289(17): 11906-11915.
| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 394.47 |
| Cas No. | 1401223-22-0 |
| Formula | C22H26N4O3 |
| Solubility | insoluble in H2O; ≥4.44 mg/mL in EtOH with ultrasonic; ≥70.7 mg/mL in DMSO |
| Chemical Name | N-isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide |
| SDF | Download SDF |
| Canonical SMILES | CCCC1=CC=C(OCC(N(C(C)C)CC2=NC(C3=CN=CC=C3)=NO2)=O)C=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | PI-1840是一种可逆的和选择性的胰凝乳蛋白酶样(CT-L)抑制剂,IC50值为27 nM. | |||||
| 靶点 | CT-L | |||||
| IC50 | 27 nM | |||||
质量控制和MSDS
- 批次:
化学结构
