化合物 PI1840|T6941|TargetMol

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發(fā)貨地	上海
更新日期	2026-06-29

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產(chǎn)品詳情

中文名稱(chēng):化合物 PI1840	英文名稱(chēng):PI-1840
CAS:1401223-22-0	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 99.50%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T001\|T6941

Product Introduction

Bioactivity

名稱(chēng)	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).
細(xì)胞實(shí)驗(yàn)	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)
激酶實(shí)驗(yàn)	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.
體外活性	PI-1840在完整的人類(lèi)MDA-MB-468癌細(xì)胞中強(qiáng)效抑制蛋白酶體CT-L活性，其IC50為0.37 μM，并抑制人類(lèi)MDA-MB-468細(xì)胞的增殖/存活。[1] 在完整的癌細(xì)胞中，PI-1840抑制CT-L活性，誘導(dǎo)蛋白酶體底物p27、Bax和IκB-α的積累，抑制存活途徑和活性，并誘導(dǎo)凋亡。[2]
體內(nèi)活性	PI-1840 (150 mg/kg i.p.) 在小鼠中抑制了MDA-MB-231乳腺腫瘤的生長(zhǎng)。[2]
存儲(chǔ)條件	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.
關(guān)鍵字	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
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相關(guān)庫(kù)	抑制劑庫(kù) \| 抗乳腺癌化合物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 高選擇性抑制劑庫(kù) \| 抗衰老化合物庫(kù) \| HIF-1化合物庫(kù) \| 抗卵巢癌化合物庫(kù) \| NO PAINS 化合物庫(kù) \| 表觀(guān)遺傳庫(kù) \| 血液病分子庫(kù) \| 免疫/炎癥分子化合物庫(kù)

關(guān)鍵字： PI 1840;TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專(zhuān)業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶(hù)群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿(mǎn)足不同需求的化合物庫(kù)，以及多種類(lèi)型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類(lèi)多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿(mǎn)足客戶(hù)的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專(zhuān)業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （14年）	注冊(cè)資本	566.265100萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
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公司成立：14年
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