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。PR-619 可诱导内质网应激和内质网应激相关的凋亡。
| 生物活性 | PR-619 is a broad-range and reversibleDUBinhibitor withEC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM forUSP4,USP8,USP7,USP2, andUSP5, respectively. PR-619 induces ER Stress and ER-Stress relatedapoptosis[1][2][3][4]. |
| IC50& Target | 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
(In Vitro) | PR-619, a deubiquitylase inhibitor, prevents degradation, indicating KCa3.1 is targeted for degradation by ubiquitylation[2].
PR-619 affects the microtubule network and led to the accumulation of small punctuated tau deposits around. PR-619 causes the dephosphorylation of tau[3].
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[3].
PR-619 (9 μM) affects the organization of the microtubule network in OLN-t40 cells[3].
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[4].
Cell Cytotoxicity Assay[1] | 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. |
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体内研究
(In Vivo) | PR-619 (10 mg/kg/day) enhances the antitumor effect of Cisplatin on a Cisplatin-Naive and Cisplatin-resistant UC Xenograft of nude mice[4].
| Animal Model: | Nude mice[4]. | | Dosage: | 10 mg/kg/day (Cisplatin combined). | | Administration: | Intraperitoneally. | | Result: | Enhanced the antitumor effect of Cisplatin. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 21 mg/mL(94.05 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂： 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。 *以上所有助溶剂都可在本网站选购。
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