P 22077
目录号: PL03758 纯度: ≥98%
CAS No. :1247819-59-5
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PL03758-10mg 10mg ¥1253.00 请登录
PL03758-50mg 50mg ¥3786.00 请登录
PL03758-100mg 100mg ¥6107.00 请登录
PL03758-200mg 200mg 询价 询价
PL03758-500mg 500mg 询价 询价
PL03758-10mM*1mLinDMSO 10mM*1mLinDMSO ¥1379.00 请登录
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中文名称
P 22077
中文别名
1-[5-[(2,4-二氟苯基)硫基]-4-硝基-2-噻吩基]乙酮;P 22077 抑制剂
英文名称
P 22077
英文别名
P22077;1-[5-(2,4-difluorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone;1-[5-[(2,4-Difluorophenyl)thio]-4-n-itro-2-thienyl]-ethanone;P-22077;P 22077
Cas No.
1247819-59-5
分子式
C12H7NO3F2S2
分子量
315.32
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
P 22077 是一种泛素蛋白特异性蛋白酶 (USP7) 抑制剂,EC50 值为 8.01 μM,同时可抑制 USP47,EC50 值为 8.74 μM。
生物活性
P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC 50 of 8.01 μM. P 22077 also inhibits USP47 with an EC 50 of 8.74 μM.
性状
Solid
IC50 & Target[1][2]
EC50: 8.01 μM (USP7), 8.74 μM (USP47)
体外研究(In Vitro)
P 22077 is an inhibitor of USP7 and DUB USP47, with EC50s of 8.01 μM and 8.74 μM, respectively. P 22077 (15-45 μM) inhibits a much smaller subset of DUBs. P 22077 (25 μM) causes DUBs inhibition in HEK293T cells. P 22077 (0-20 μM) greatly reduces the cell viability of Neuroblastoma (NB) cells including IMR-32, NGP, CHLA-255, and SH-SY5Y cells but without NB-19 and SK-N-AS cells. P 22077 (10 μM) increases p53 activity and induces apoptosis in p53 wild-type and HDM2-expressing NB cells. P 22077 (5 μM) enhances the cytotoxic effect of Dox and VP-16 on NB cells, and enhances Dox- and VP-16-induced p53-mediated apoptosis. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
P 22077 (15?mg/kg, i.p. 21 days) shows potent antitumor activities in an xenograft mouse model bearing IMR-32-derived tumors; P 22077 also exhibits antitumor effects after treatment at 10?mg/kg for 14 days in mice bearing SH-SY5Y-derived tumors, and at 20 mg/kg for 12 days in mice bearing NGP-derived tumors. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Altun M, et al. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol. 2011 Nov 23;18(11):1401-12.
[2]. Fan YH, et al. USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis. Cell Death Dis. 2013 Oct 17;4:e867.
溶解度数据
In Vitro: DMSO : 50 mg/mL (158.57 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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