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2,6-二氨基-3,5-二硫氰基吡啶

2,6-二氨基-3,5-二硫氰基吡啶用途

PR-619 是一种 DUB 抑制剂,作用于 USP4,USP8,USP7,USP2 和 USP5,EC50 分别为 3.93,4.9,6.86,7.2 和 8.61 μM。

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2,6-二氨基-3,5-二硫氰基吡啶名称

[ CAS 号 ]:
2645-32-1

[ 中文名 ]:
2,6-二氨基-3,5-二硫氰基吡啶

[ 英文名 ]:
PR-619

[英文别名 ]:

2,6-Diaminopyridine-3,5-bis(thiocyanate)
2,6-diamino-5-(cyanothio)pyridin-3-yl thiocyanate
Thiocyanic acid,2,6-diamino-3,5-pyridinediyl ester
3,5-bis-thiocyanato-pyridine-2,6-diamine
HMS1440E01
2,6-Diamino-3,5-dithiocyanato-pyridin
2,6-diamino-3,5-bis(thiocyanato)pyridine
QC-8206
2,6-Diamino-3,5-pyridinediyl bis(thiocyanate)
3,5-dithiocyanatopyridine-2,6-diamine

2,6-二氨基-3,5-二硫氰基吡啶生物活性

[ 描述 ]:

PR-619 是一种 DUB 抑制剂,作用于 USP4,USP8,USP7,USP2 和 USP5,EC50 分别为 3.93,4.9,6.86,7.2 和 8.61 μM。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 去泛素化酶

研究领域 >> 癌症

[ 靶点 ]

EC50: 3.93 μM (USP4), 4.9 μM (USP8), 6.86 μM (USP7), 7.2 μM (USP2), 8.61 μM (USP5)[1]

[体外研究]

PR-619,一种去泛素化酶抑制剂,可防止降解,表明KCa3.1是通过泛素化降解的目标。在PR-619处理的细胞中,通道降解受到显着抑制,24小时后仍然存在87±1％的KCa3.1(n = 3; P <0.05)[2]。通过MTT测定确定细胞活力,并揭示PR-619在7-10μM的非常窄的浓度范围内发挥浓度依赖性细胞毒性[3]。

[激酶实验]

将20mM Tris-HCl，pH8.0,2mM CaCl2和2mMβ-巯基乙醇（DUB测定缓冲液）中的重组酶与单剂量或剂量范围的PR-619或P22077在96孔板中预孵育30分钟。添加Ub-PLA2和NBD C6-HPC。使用Perkin Elmer Envision荧光板读数器在室温下监测在测定的线性范围内荧光产物的释放。包含载体（2％（v / v）DMSO）和10mM N-乙基马来酰亚胺作为对照。当观察到≥60％抑制时，使用S形剂量响应方程确定EC 50值。类似的测定方案用于测量其他体外酶测定活性[1]。

[细胞实验]

确定生长抑制，除了在补充有10％（v / v）FBS，1％（v / v）青霉素/链霉素和2mM L-谷氨酰胺的DMEM中维持的HCT-116或HEK293T细胞暴露于剂量范围PR-619（1,5,10,20和50μM）或P22077持续72小时[1]。

[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]. Bertuccio CA, et al. Anterograde trafficking of KCa3.1 in polarized epithelia is Rab1- and Rab8-dependent and recycling endosome-independent. PLoS One. 2014 Mar 14;9(3):e92013.

[3]. Seiberlich V, et al. The small molecule inhibitor PR-619 of deubiquitinating enzymes affects the microtubule network and causes protein aggregate formation in neural cells: implications for neurodegenerative diseases. Biochim Biophys Acta. 2012 Nov;1823(1

[相关活性小分子]

BAY 11-7082 | P005091 | VLX1570 | (2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺 | 1-[5-[(2,4-二氟苯基)硫基]-4-硝基-2-噻吩基]乙酮 | 的DUB-IN-2 | ML364 | (3E,5E)-3,5-二[(4-硝基苯基)亚甲基]-1-(1-氧代-2-丙烯-1-基)-4-哌啶酮 | GEN6776 | ML-323 | HBX 19818 | 1-[1-(4-氟苯基)-2,5-二甲基-1H-吡咯-3-基]-2-(1-吡咯烷基)乙酮 | LDN-57444 | 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

2,6-二氨基-3,5-二硫氰基吡啶物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
406.0±45.0 °C at 760 mmHg

[ 熔点 ]:
210℃

[ 分子式 ]:
C₇H₅N₅S₂

[ 分子量 ]:
223.278

[ 闪点 ]:
199.3±28.7 °C

[ 精确质量 ]:
222.998642

[ PSA ]:
163.84000

[ LogP ]:
2.05

[ 外观性状 ]:
white to beige

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.764

[ 储存条件 ]:
?20°C

[ 水溶解性 ]:
DMSO: soluble5mg/mL (clear solution)

2,6-二氨基-3,5-二硫氰基吡啶MSDS

详细MSDS(安全技术说明书)

2,6-二氨基-3,5-二硫氰基吡啶安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H315-H317-H318-H335

[ 警示性声明 ]:
P261-P280-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-37/38-41-43

[ 安全声明 (欧洲) ]:
26-36/37/39

[ 危险品运输编码 ]:
NONH for all modes of transport

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2,6-二氨基-3,5-二硫氰基吡啶文献

Development of two novel high-throughput assays to quantify ubiquitylated proteins in cell lysates: application to screening of new anti-malarials.

Malaria Journal 14 , 200, (2015)

The ubiquitin proteasome system (UPS) is one of the main proteolytical pathways in eukaryotic cells and plays an essential role in key cellular processes such as cell cycle, stress response, signal tr...

Inflammasomes-dependent regulation of IL-1β secretion induced by the virulent Mycobacterium bovis Beijing strain in THP-1 macrophages.

Antonie van Leeuwenhoek 108 , 163-71, (2015)

Mycobacterium bovis is the causative agent of tuberculosis in cattle. Infection of macrophages with M. bovis leads to the activation of the "nucleotide binding and oligomerization, leucine-rich repeat...

Screening of DUB activity and specificity by MALDI-TOF mass spectrometry.

Nat. Commun. 5 , 4763, (2014)

Deubiquitylases (DUBs) are key regulators of the ubiquitin system which cleave ubiquitin moieties from proteins and polyubiquitin chains. Several DUBs have been implicated in various diseases and are ...

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