|2,6-二氨基-3,5-二硫氰基吡啶|CsnPharm

CAS No.: 2645-32-1

PR-619 Catalog No. CSN13807

Synonyms: 2,6-Diamino-3,5-dithiocyanopyridine;DUB Inhibitor V

PR-619 is a broad-spectrum and reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM and it was developed for chemotherapy.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 DUB

EC50:1-20μM
描述Deubiquitinating enzymes (DUBs) remove ubiquitin from their substrates and, together with ubiquitin ligases, play an important role in the regulation of protein expression. PR-619 is a broad-range UDB inhibitor that led to cell morphological changes, the upregulation of HSPs and accumulation of ubiquitinated protein species. PR-619 exhibits concentration dependent cytotoxicity in very narrow concentration range of 7 - 10 μM to OLN 93 cells. Treatment with 9 μM PR-619 causes an increase in the abundance of ubiquitinated protein, and proteasomal activity reduce to 50% within 24 h. PR-619 promotes the association of tau, ubiquitin and p62 with microtubules and alter their solubility^[3]. In addition, Treatment with the PR-619 increased caspase-8 ubiquitination and caspase-8 enzymatic activity and sensitized normal fibroblasts to TRAIL-mediated apoptosis^[4]. In vivo, administered daily with 100 μg PR-619 improves renal histopathological changes in mice with unilateral ureteral obstruction. Administration of PR-619 also attenuated renal fibrosis with downregulation of mesenchymal markers, extracellular matrix proteins, matrix metalloproteinases, apoptosis, macrophage infiltration, and the TGF-β1 mRNA level^[5].
动物研究
剂量
Mice: 10 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.4787 mL
- 22.3936 mL
- 44.7872 mL
- 5 mM
- 0.8957 mL
- 4.4787 mL
- 8.9574 mL
- 10 mM
- 0.4479 mL
- 2.2394 mL
- 4.4787 mL

技术信息

CAS号

2645-32-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C7H5N5S2

运输

蓝冰

分子量

223.28

别名

2,6-Diamino-3,5-dithiocyanopyridine;DUB Inhibitor V

溶解度

DMSO	22.0 mg/mL (98.5 mM) warming
Water	insoluble

动物实验配方

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