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CAS No.: 1247819-59-5

P 22077 Catalog No. CSN13634

Synonyms: P22077

P22077 is an inhibitor of ubiquitin specific protease USP7 (EC50 = 8.6 μM). P22077 also inhibits the deubiquitinase USP47.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 USP7

EC50:8.6μM
描述Deubiquitinating enzymes (DUBs) function to remove covalently attached ubiquitin from proteins, thereby controlling substrate activity and/or abundance. More than the half of DUBs belong to the ubiquitin-specific protease (USP) subfamily. USP7 is the most widely studied DUB and is well known as herpes-associated USP (HAUSP). USP7 can influence the location, activation , and stability of its substrates^[3]. P22077 is an inhibitor of USP7 with IC50 value of 6 and 10 μM for USP10 and USP7, respectively^[4]. In vitro, P22077 activates p53 and its targeted gene p21 (cyclin-dependent kinase inhibitor 1) in human colon carcinoma HCT116 cells. P22077 greatly reduced the cell viability and induced apoptosis of IMR-32, NGP, CHLA-255, and SH-SY5Y cells but not that of NB-19 and SK-N-AS cells at concentration ranging in 1 - 20 μM. P22077 stabilized p53 by inducing HDM2 protein degradation, and augmented the cytotoxic effects of doxorubicin and etoposide in neuroblastoma cells. In vivo, administration P2207 at dose of 15 mg/kg daily for 3 weeks significantly inhibited tumor growth in the orthotopic neuroblastoma mouse model^[5]. Treatment with P2207 on the dose of 20 mg/kg daily for 30 days significantly suppressed the growth of MYCN-amplified human neuroblastoma cell lines in xenograft mouse models^[6].
作用机制P22077 covalently modify the catalytic cysteine of USP7 and induce a conformational switch in the enzyme associated with active site rearrangement^[7].
动物研究
剂量
SCID mice: 30 mg/kg^[3] (i.p.), 10 mg/kg - 20 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	SCID mice: 30 mg/kg^[3] (i.p.), 10 mg/kg - 20 mg/kg^[4] (i.p.)
给药途径	i.p.

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
- 3.1714 mL
- 15.8571 mL
- 31.7142 mL
- 5 mM
- 0.6343 mL
- 3.1714 mL
- 6.3428 mL
- 10 mM
- 0.3171 mL
- 1.5857 mL
- 3.1714 mL

技术信息

CAS号

1247819-59-5

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H7F2NO3S2

运输

蓝冰

分子量

315.32

别名

P22077

溶解度

DMSO	63.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

2% DMSO+30% PEG 300+2% Tween 80+water

3 mg/mL

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