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别名 | N/A | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C7H5N5S2 |
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分子量 | 223.28 | CAS号 | 2645-32-1 | |
Solubility (25°C)* | 体外 | DMSO | 4 mg/mL (17.91 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
产品描述 | PR-619 是一种非选择性的 deubiquitinylating enzymes (DUBs) 可逆抑制剂,无细胞试验中EC50为1-20 μM。PR-619 可激活自噬。 | |||||||||||
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靶点 |
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体外研究 | PR-619是可渗透细胞的,吡啶类广谱DUB抑制剂,靶向作用于ATXN3, BAP1, JOSD2, OTUD5, UCH-L1, UCH-L3, UCH-L5/UCH37, USP1, 2, 4, 5, 7, 8, 9X, 10, 14, 15, 16, 19, 20, 22, 24, 28, 47, 48, VCIP135, YOD1, 及deISGylase PLpro, deNEDDylase DEN1, 和deSUMOlyase SENP6。PR-619作用于HEK293T细胞,提高整体的蛋白质泛素化,这种作用存在剂量和时间依赖性(20到150μM,0.5到20小时)。PR619处理,上调K48和K63连接的多聚泛素链。PR-619诱导HCT116细胞死亡,EC50为6.3 μM。[1] |
激酶实验 | Ub-PLA2 实验 | |
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20 mM Tris-HCl, pH 8.0,2 mM CaCl2 和2 mM β-巯基乙醇(DUB 实验 buffer)中的重组酶与PR-619或P22077在96孔板中预温育30分钟,然后加入Ub-PLA2和NBD C6-HPC。在室温下使用荧光酶标仪监测线性范围内释放的荧光产物。空白组(2%(v/v) DMSO)和10 mM N-ethylmaleimide作为对照。观察到抑制≥60%,使用S形曲线剂量反应方程测定EC50值。 | ||
细胞实验 | 细胞系 | HCT116, HEK293T |
浓度 | 0.5-50 μM | |
处理时间 | 72 小时 | |
方法 | 72小时后, 每孔加入在PBS中制备的0.2 mg/mL Resazurin,细胞再温育3-6小时。使用Ex=535 nm 和Em=590 nm过滤器在荧光计上测量Resazurin还原产物的荧光值。使用Prism计算 EC50值。 |
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数据来源于[Data independently produced by , , Front Pharmacol, 2017, https://doi.org/10.3389/fphar.2017.00565]
数据来源于[Data independently produced by , , Front Pharmacol, 2018, 8:565]
数据来源于[Data independently produced by , , Anim Reprod Sci, 2017, 187:64-73]
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