化合物 PI1840|T6941|TargetMol

PI-1840
1401223-22-0

￥145 1mg 起订

￥330 5mg 起订

￥537 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 PI1840

英文名称：: PI-1840

CAS号：: 1401223-22-0

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 100%

产品类别：: 抑制剂

货号：: T6941

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.
溶解度	Ethanol : 31 mg/mL (78.6 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 72 mg/mL (182.5 mM)
关键字	cell proliferation \| Proteasome \| Caspase \| proteasome substrates \| poly ADP ribose polymerase \| inhibit \| NF-κB \| Autophagy \| cell cycle \| PI1840 \| anticancer \| Apoptosis \| Bcl-2 Family \| MG-63 cells \| Nuclear factor-kappaB \| PI-1840 \| Inhibitor \| U2-OS cells \| PARP \| Nuclear factor-κB
相关产品	Niraparib \| XAV-939 \| Olaparib \| Sitagliptin \| 3-Aminobenzamide \| Benzamide \| Anagliptin \| Alloxan monohydrate \| Sitagliptin phosphate monohydrate \| 4'-Hydroxychalcone \| Vildagliptin \| Linagliptin
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 细胞凋亡化合物库 \| 高选择性抑制剂库 \| 抗衰老化合物库 \| 蛋白酶抑制剂库 \| NO PAINS 化合物库 \| DNA 损伤和修复分子库 \| 表型筛选靶点鉴定库

PI 1840|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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