GlpBio

PR-619

目录号: GC13208纯度: >98.00%同义词: 2,6-二氨基-3,5-二硫氰基吡啶
PR-619是一种广谱的去泛素酶抑制剂。
PR-619
Cas No.: 2645-32-1
规格价格库存数量操作
1mg¥139.00现货
1
5mg¥299.00现货
1
10mg¥479.00现货
1
25mg¥773.00现货
1
50mg¥1,050.00现货
1
100mg¥1,680.00现货
1
200mg¥2,599.00现货
1
10mM (in 1mL DMSO)¥342.00现货
1
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产品描述 Description

PR-619 is a broad-spectrum DUB (deubiquitinating enzyme) inhibitor. PR-619 has demonstrated robust DUB inhibitory activity (5-20 µM) and growth inhibitory activity with IC50 of 2 µM in HEK 293T cells[1].

PR-619 at 40 µM induced an above-background TOP2A and TOP2B signal in K562 cells[2]. In vitro efficacy test shown that the anti-tumor effects of PR-619 on the JJ012 and SW1353 human chondrosarcoma cell lines, with PR-619 concentrations ranging from 2.5 to 17.5 µM for 24 and 48 h. PR-619 significantly reduced the viability of chondrosarcoma cells in a dose- and time-dependent manner[3]. In vitro, PR-619 treatment (0 - 80 µM) significantly inhibited cell viability at 24 and 48 h in a dose-dependent manner. Furthermore, PR-619 (20 µM) treatment for 48 h significantly induced apoptosis in cisplatin-resistant T24/R cells[4].

In vivo, mice were intraperitoneally treated with PR-619 (10 mg/kg each day) enhanced the antitumor effect of cisplatin in a xenograft mouse model of T24/R[4].

References:
[1] Altun M, et al. (2011) Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol 18:1401-1412
[2] Cowell IG, et al. The Deubiquitinating Enzyme Inhibitor PR-619 is a Potent DNA Topoisomerase II Poison. Mol Pharmacol. 2019 Nov;96(5):562-572.
[3] Lin WC, et al. Anti-tumor effects of deubiquitinating enzyme inhibitor PR-619 in human chondrosarcoma through reduced cell proliferation and endoplasmic reticulum stress-related apoptosis. Am J Cancer Res. 2023 Jul 15;13(7):3055-3066.
[4] Hsu FS, et al. PR-619, a General Inhibitor of Deubiquitylating Enzymes, Diminishes Cisplatin Resistance in Urothelial Carcinoma Cells through the Suppression of c-Myc: An In Vitro and In Vivo Study. Int J Mol Sci. 2021 Oct 28;22(21):11706.

PR-619是一种广谱的去泛素酶抑制剂。PR-619在HEK 293T细胞中表现出强大的DUB抑制活性(5-20µM)和生长抑制活性,IC50为2µM[1]。

40µM的PR-619在K562细胞中诱导高于背景的TOP2A和TOP2B信号[2]。体外疗效测试显示,PR-619对JJ012和SW1353人软骨肉瘤细胞系的抗肿瘤作用,PR-6119浓度范围为2.5至17.5 µM,持续24和48小时。PR-619以剂量和时间依赖的方式显著降低软骨肉瘤细胞的生存能力[3]。在体外,PR-619处理(0-80µM)在24和48小时以剂量依赖的方式显著抑制细胞活力。此外,PR-619(20µM)处理48小时可显著诱导顺铂耐药T24/R细胞凋亡[4]。在体内,用PR-619(每天10 mg/kg)腹膜内处理小鼠,增强了T24/R异种移植小鼠模型中顺铂的抗肿瘤作用[4]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Preparation Method

T24 and BFTC-905 cells were treated with various concentrations of PR-619 (3-15 µM) for 24 h, 48 h, and 72 h, respectively. Cell viability was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.

Reaction Conditions

3-15 µM；24 h, 48 h, and 72 h

Applications

PR-619 effectively induced cytotoxicity and apoptosis in both T24 and BFTC cells in a dose- and time-dependent manner. Additionally, we found that PR-619 induced cytotoxicity in low-grade RT-4 UC cells and cisplatin-resistant UC cells (T24/R) in a dose- and time-dependent manner.
Animal experiment [2]:

Animal models

8-week-old male nude mice

Preparation Method

A total of 5 × 105 JJ012 or SW1353 cells were suspended in 200 µL of serum-free medium and an equal amount of Matrigel. The cell suspension thus derived was then injected subcutaneously into the dorsal side of 8-week-old male nude mice. When the tumor grew to ~150 mm3, mice were randomly assigned to either the PR-619 treatment group or the control group. Mice in the treatment group received PR-619 10 mg/kg intraperitoneal injection twice daily for 48 days. Mice in the untreated control group received an injection of DMSO solution.

Dosage form

10 mg/kg; i.p.

Applications

PR-619 showed significant anti-tumor effects on xenograft tumors from both cell lines.

References:

[1] Kuo KL, et al. The Deubiquitinating Enzyme Inhibitor PR-619 Enhances the Cytotoxicity of Cisplatin via the Suppression of Anti-Apoptotic Bcl-2 Protein: In Vitro and In Vivo Study. Cells. 2019 Oct 17;8(10):1268.
[2] Lin WC, et al. Anti-tumor effects of deubiquitinating enzyme inhibitor PR-619 in human chondrosarcoma through reduced cell proliferation and endoplasmic reticulum stress-related apoptosis. Am J Cancer Res. 2023 Jul 15;13(7):3055-3066.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
2645-32-1
同义词
2,6-二氨基-3,5-二硫氰基吡啶
化学名
(2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate
SMILES
C1=C(C(=NC(=C1SC#N)N)N)SC#N
分子式
C7H5N5S2
分子量
223.28 g/mol
溶解性
≥ 11.15mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol