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PI-1840
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PI-1840图片
CAS NO:1401223-22-0
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
PI-1840 是一种有效的选择性糜蛋白酶样 (CT-L) 抑制剂，IC50 值为 27 nM。 PI-1840 抑制细胞增殖并将细胞周期阻滞在 G2/M 期。 PI-1840 诱导细胞凋亡并诱导自噬。 PI-1840 诱导蛋白酶体底物 p27、Bax 和 IκB-α 的积累。
Cas No.1401223-22-0
化学名N-isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide
Canonical SMILESCCCC1=CC=C(OCC(N(C(C)C)CC2=NC(C3=CN=CC=C3)=NO2)=O)C=C1
分子式C22H26N4O3
分子量394.47
溶解度≥ 70.7mg/mL in DMSO
储存条件Desiccate at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PI-1840 is a potent and selective inhibitor of proteasome with IC50 value of 27 nM for chymotrypsinlike (CT-L) activity [1].

The 26S proteasome consists of a 19S regulatory particle (RP) and a 20S core particle. The 26S proteasome have three main catalytic activities: chymotrypsin-like (CT-L), peptidylglutamyl peptide hydrolyzing-like (PGPH-L) and trypsin-like (T-L) activities. CT-L activity plays an important role in the degradation of tumor suppressor and apoptotic proteins [1].

PI-1840 is a rapidly reversible and non-covalent proteasome CT-L inhibitor. PI-1840 exhibited excellent selectivity for CT-L over PGPH-L and T-L activities. In MDA-MB-468 human breast cancer cells, PI-1840 inhibited the CT-L activity with IC50 value of 0.37 μM and inhibited cell survival/proliferation [1]. Also, PI-1840 exhibited 121-fold selectivity for the constitutive 20 S proteasome over the immunoproteasome with IC50 values of 18 and 2170 nM, respectively. In MDA-MB-468 cells, PI-1840 caused the accumulation of CT-L substrates IκB-α, p27 and Bax. Also, PI-1840 reduced the levels of survivin, p-Akt and Ser(P)-6 and induced apoptosis through poly(ADP-ribose) polymerase cleavage and caspase-3 activation [2].

In nude mice bearing human breast tumor, PI-1840 (150 mg/kg/day, i.p, daily) inhibited tumor growth by 85% [2].

References:
[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.