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PR-619

去泛素化酶（DUBs）抑制剂,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。

目录号: PC16215 纯度: ≥98%

CAS No. :2645-32-1

商品编号	规格	价格	会员价
PC16215-5mg	5mg	¥392.00	请登录
PC16215-25mg	25mg	¥980.00	请登录
PC16215-100mg	100mg	¥2744.00	请登录
PC16215-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥784.00	请登录

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中文名称

PR-619

中文别名

2,6-二氨基-3,5-二硫氰基吡啶;2,6-二氨基-3,5-二硫代氰基吡啶;3-氨基联苯-d9;PR-619 抑制剂

英文名称

3,5-Dithiocyanatopyridine-2,6-diamine

英文别名

PR 619;PR-619;(2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate;2,?6-?Diamino-?3,?5-?dithiocyanopyridine;3,5-Bis-thiocyanato-pyridine-2,6-diamine;3,5-dithiocyanatopyridine-2,6-diamine;PR-619 (PR 619);2,6-diamino-3,5-bis(thiocyanato)pyridine;2,6-Diamino-3,5-dithiocyanato-pyridin;2,6-Diamino-3,5-dithiocyanopyridine;2,6-Diaminopyridine-3,5-bis(thiocyanate);HMS1440E01;QC-8206;Thiocyanic acid,2,6-diamino-3,5-pyridinediyl ester;Thiocyanic acid C,C′-(2,6-diamino-3,5-pyridinediyl) ester;Thiocyanic acid C,C′-(2,6-diamino-3,5-pyridinediyl) ester; 2,6-Diaminopyridine-3,5-bis(thiocyanate);Thiocyanic acid, 2,6-diamino-3,5-pyridinediyl ester;AK161038;Maybridge3_003257;AOB1115;HMS3653C09;JFD01947;BCP07903;s7130;FCH2295945;IDI1_014644;2,6-Diamino-3,5-bisthiocyanatopyridine

Cas No.

2645-32-1

分子式

C₇H₅N₅S₂

分子量

223.28

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

PR-619 is a broad-range and reversible DUB inhibitor with EC₅₀s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis.

性状

Solid

IC50 & Target[1][2]

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

体外研究(In Vitro)

PR-619, a deubiquitylase inhibitor, prevents degradation, indicating KCa3.1 is targeted for degradation by ubiquitylation.
PR-619 affects the microtubule network and led to the accumulation of small punctuated tau deposits around. PR-619 causes the dephosphorylation of tau.
PR-619 (7-12.5 μM) causes an increase in the abundance of ubiquitinated proteins within 24 h. PR-619 leads to the induction of heat shock proteins and to an increase of ubiquitinated proteins.
PR-619 (9 μM) affects the organization of the microtubule network in OLN-t40 cells.
PR-619 (5, 7.5, and 10 μM) induces ER Stress and ER-Stress related apoptosis on T24 and BFTC-905 cells. PR-619 induces polyubiquitination, Bcl-2 downregulation, and concurrent PARP cleavage in a dose-dependent manner. PR-619 induces G0/G1 arrest in UC cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay

Cell Line:	OLN-t40 cells.
Concentration:	0-10 μM.
Incubation Time:	24 hours.
Result:	Exerted concentration-dependent cytotoxicity in a very narrow concentration range of 7-10 μM.

体内研究(In Vivo)

PR-619 (10 mg/kg/day) enhances the antitumor effect of Cisplatin on a Cisplatin-Na?ve and Cisplatin-resistant UC Xenograft of nude mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice.
Dosage:	10 mg/kg/day (Cisplatin combined).
Administration:	Intraperitoneally.
Result:	Enhanced the antitumor effect of Cisplatin.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

[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 [Information]

[4]. Kuan-Lin Kuo, et al. The Deubiquitinating Enzyme Inhibitor PR-619 Enhances the Cytotoxicity of Cisplatin via the Suppression of Anti-Apoptotic Bcl-2 Protein: 体外研究 and In Vivo Study. Cells. 2019 Oct 17;8(10):1268. [Information]

溶解度数据

体外研究:

DMSO : ≥ 21 mg/mL (94.05 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.4787 mL	22.3934 mL	44.7868 mL
5 mM	0.8957 mL	4.4787 mL	8.9574 mL
10 mM	0.4479 mL	2.2393 mL	4.4787 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (11.20 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (11.20 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液

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产品使用指南

Data Sheet

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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