貨號	規格	價格	上海	北京	武漢	南京
S80324-5mg	99.2%	￥330.00 S80324-5mg ￥330.00 現貨	5 5	-	-	-
S80324-10mg	99.2%	￥530.00 S80324-10mg ￥530.00 現貨	5 5	-	-	-
S80324-25mg	99.2%	￥1050.00 S80324-25mg ￥1050.00 現貨	5 5	-	-	-
S80324-100mg	99.2%	￥2860.00 S80324-100mg ￥2860.00 現貨	3 3	-	-	-

產品介紹

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).

產品描述：

靶點：

Proteasome;PARP;PARP;Proteasome

體外研究：

PI-1840 potently inhibits proteasomal CT-L activity with IC50 of 0.37 μM in intact human MDA-MB-468 cancer cells, and inhibits proliferation/survival of human MDA-MB-468 cells. [1] In intact cancer cells, PI-1840 inhibits CT-L activity, induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis.

體內研究：

PI-1840 (150 mg/kg i.p.) inhibits the tumor growth in mice of MDA-MB-231 breast tumors.

細胞實驗：

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)

參考文獻：

1. Kazi A, Ozcan S, Tecleab A, Sun Y, Lawrence HR, Sebti SM. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem. 2014;289(17):11906-11915. doi:10.1074/jbc.M113.533950. 2. Ozcan S, et al. Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors. J Med Chem. 2013, 56(10), 3783-3805.

溶解性：

Soluble in DMSO、Ethanol

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.535 ml	12.675 ml	25.351 ml
5 mM	0.507 ml	2.535 ml	5.07 ml
10 mM	0.254 ml	1.268 ml	2.535 ml
50 mM	0.051 ml	0.254 ml	0.507 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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PI-1840

N-isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide