|1-(5-((2,3-二氯苯基)硫基)-4-硝基噻吩-2-基)乙烷-1-酮|CsnPharm

CAS No.: 882257-11-6

1-(5-((2,3-Dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethan-1-one Catalog No. CSN16620

Synonyms: P5091

P005091 acts as a selective inhibitor of ubiquitin-specific protease 7 (USP7) and USP47 with the EC50s of 4.2 μM and 4.3 μM respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 USP7

EC50:4.2μM
描述Deubiquitylating enzymes (DUBs) antagonize the ubiquitylation of substrates by cleaving mono and polyubiquitin and thus afford an additional level of post-translational regulation. USP7 (Ubiquitin-specific protease 7) is a deubiquitinase that has activity on numerous targets, including the E3 ligase MDM2^[3]. P00591 is a selective inhibitor of USP7 and USP47 activity with IC50 values of 4.2 μM and 4.3 μM^[4]. P005091 stabilizes p53, inhibits cancer cell proliferation, and is active in cellular models of disease. In vitro, P005091 accelerated the degradation of the USP7 substrate HDM2 in several cancer cell lines, inhibited the growth of HCT-116 human colorectal cancer cells with an IC50 of 11 μM, and inhibited cancer cell growth synergistically with doxorubicin, etoposide, or mechlorethamine^[4]. In vivo, P00591 decreased expression of PCNA and triggered cleavage of PARP and caspase-3 in a dose-dependent manner. Administration of P00591 at 10 mg/kg leaded to enhanced proliferation inhibition and apoptosis in tumor tissues in mouse colon cancer CT26 cells xenograft mice. Treatment with 10 mg/kg P005091 promoted the CD4⁺ and CD9⁺ T-cell-mediated antitumor immune response, and inhibited FOXP3⁺ Treg function in CT26 cells xenograft mice^[5].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human HCT116 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs, EC50=11 μM	24900381
Sf9 cells	-	Function assay	-	Inhibition of recombinant USP7 expressed in Sf9 cells by Ub-CHOP reporter assay, EC50=4.2 μM	24900381

动物研究
剂量
Mice: 5 mg/kg, 10 mg/kg^[3] (i.p.), 15 mg/kg - 25 mg/kg^[4] (i.p.); 10 mg/kg^[1] (i.v.)

给药途径
i.p., i.v.

动物研究
剂量	Mice: 5 mg/kg, 10 mg/kg^[3] (i.p.), 15 mg/kg - 25 mg/kg^[4] (i.p.); 10 mg/kg^[1] (i.v.)
给药途径	i.p., i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8717 mL
- 14.3585 mL
- 28.7171 mL
- 5 mM
- 0.5743 mL
- 2.8717 mL
- 5.7434 mL
- 10 mM
- 0.2872 mL
- 1.4359 mL
- 2.8717 mL

技术信息

CAS号

882257-11-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H7Cl2NO3S2

运输

蓝冰

分子量

348.22

别名

P5091

溶解度

DMSO	33.0 mg/mL (94.8 mM) warming
Water	insoluble

动物实验配方

IP	3% DMSO+2% Tween80+40% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	65 mg/mL	suspension

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1-(5-((2,3-Dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethan-1-one Catalog No. CSN16620

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