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4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺

更新时间:2024-01-10 17:46:25

4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺结构式
4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺结构式
品牌特惠专场
常用名 4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺 英文名 USP7/USP47 inhibitor
CAS号 1247825-37-1 分子量 484.39900
密度 N/A 沸点 N/A
分子式 C18H11Cl2N3O3S3 熔点 N/A
MSDS N/A 闪点 N/A

 用途


USP7/USP47 inhibitor 是一种选择性的泛素蛋白特异性蛋白酶 7/47 (USP7/USP47) 抑制剂,EC50 值分别为 0.42 μM 和 1.0 μM。

 名称

中文名 4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺
英文名 4-Cyano-5-[(3,5-dichloro-4-pyridinyl)sulfanyl]-N-[4-(methylsulfon yl)phenyl]-2-thiophenecarboxamide
英文别名 更多

 生物活性

描述 USP7/USP47 inhibitor 是一种选择性的泛素蛋白特异性蛋白酶 7/47 (USP7/USP47) 抑制剂,EC50 值分别为 0.42 μM 和 1.0 μM。
相关类别
靶点

EC50: 0.42 μM (USP7), 1.0 μM (USP47)[1]

体外研究 USP7/USP47抑制剂(化合物14)是USP7/USP47的选择性抑制剂,EC50分别为0.42μM和1μM。 USP7/USP47抑制剂不抑制半胱天冬酶3,钙蛋白酶1,20S蛋白酶体和一组代表性USP(USP2,USP5,USP8,USP21和USP28; EC50>31.6μM)。 USP7/USP47抑制剂抑制HCT-116细胞的生长,EC50为7.6μM[1]。
激酶实验 使用标准分子生物学技术进行来自BL21(DE3)细菌的USP21的克隆,表达和纯化。产生USP2,USP5,USP7,USP8,USP28,USP47,Ub-PLA2(Ub-CHOP)和Ub-EKL(Ub-CHOP2)。使用半胱天冬酶3和半胱天冬酶3底物DEVD-Rh110。测量去泛素化酶,组织蛋白酶B和20S蛋白酶体胰凝乳蛋白酶样蛋白酶活性。使用类似的方案确定胱天蛋白酶3活性。简而言之,在加入DEVD-Rh110之前,将化合物(包括USP7 / USP47抑制剂)的剂量范围与半胱天冬酶3一起温育30分钟,并分别使用485nm和531nm的激发和发射最大值在荧光读板仪上读数。 caspase 3和DEVD-Rh110的最终浓度分别为2 nM和100 nM [1]。
参考文献

[1]. Weinstock J, et al. Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47. ACS Med Chem Lett. 2012 Sep 11;3(10):789-92.

 物理化学性质

分子式 C18H11Cl2N3O3S3
分子量 484.39900
精确质量 482.93400
PSA 165.33000
LogP 6.59338
储存条件 -20°C,密闭,干燥

 合成线路

~31%

4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺结构式

4-氰基-5-[(3,5-二氯...

1247825-37-1

文献:Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺结构式

4-氰基-5-[(3,5-二氯...

1247825-37-1

文献:Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺结构式

4-氰基-5-[(3,5-二氯...

1247825-37-1

文献:Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺结构式

4-氰基-5-[(3,5-二氯...

1247825-37-1

文献:Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺结构式

4-氰基-5-[(3,5-二氯...

1247825-37-1

文献:Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

~%

4-氰基-5-[(3,5-二氯-4-吡啶基)硫基]-N-[4-(甲基磺酰基)苯基]-2-噻吩甲酰胺结构式

4-氰基-5-[(3,5-二氯...

1247825-37-1

文献:Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar, K. G.; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 789 - 792,4 Title/Abstract Full Text Show Details Weinstock, Joseph; Wu, Jian; Cao, Ping; Kingsbury, William D.; McDermott, Jeffrey L.; Kodrasov, Matthew P.; McKelvey, Devin M.; Suresh Kumar; Goldenberg, Seth J.; Mattern, Michael R.; Nicholson, Benjamin ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 789 - 792

 英文别名

TERT-BUTYL 4-CYANO-4-PHENYL-1-PIPERIDINECARBOXYLATE
1-BOC-4-CYANO-4-PHENYL-PIPERIDINE
4-cyano-5-((3,5-dichloropyridin-4-yl)thio)-N-(4-(methylsulfonyl)phenyl)thiophene-2-carboxamide
N-(tert-butoxycarbonyl)-4-phenyl-4-cyanopiperidine
4-cyano-4-phenyl-piperidine-1-carboxylic acid tert-butyl ester
1-N-BOC-4-PHENYLPIPERIDINE-4-CARBONITRILE
USP7-USP47 inhibitor
1-Boc-4-phenyl-4-piperidinecarbonitrile
Tert-butyl 4-cyano-4-phenyl-piperidine-1-carboxylate
USP7/USP47 inhibitor
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