2. PROTAC Anti-infection
  3. PROTACs Enterovirus
  4. Jun15702

Jun15702 是一种靶向肠道病毒 D68 的病毒衣壳蛋白 (Capsid Protein) VP1 的 PROTAC 类降解剂，能够招募 Cereblon (CRBN) E3 连接酶并激活泛素-蛋白酶体通路。Jun15702 可抑制病毒进入，并在病毒复制的早期、中期和晚期阶段均发挥抑制作用。Jun15702 对多种野生型肠道病毒 D68 毒株具有抗病毒活性，且对耐 Pleconaril (HY-19952) 的肠道病毒 D68 变异株 rMO-VP1 F159V 也表现出亚微摩尔级的抗病毒活性。Jun15702可用于肠道病毒 D68 (EV-D68) 感染的相关研究。
(粉色: Enterovirus 配体 (HY-183010)；蓝色: Cereblon 配体 (HY-183011)；黑色: 连接子)。

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Jun15702

Jun15702 Chemical Structure

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Jun15702 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Jun15702 is a PROTAC degrader targeting the capsid protein VP1 of enterovirus D68. Jun15702 recruits the Cereblon (CRBN) E3 ligase and activates the ubiquitin-proteasome pathway. Jun15702 inhibits viral entry and exerts inhibitory effects during the early, middle and late stages of viral replication. Jun15702 exhibits antiviral activity against multiple wild-type enterovirus D68 strains, and also shows submicromolar antiviral activity against the Pleconaril (HY-19952)-resistant enterovirus D68 variant rMO-VP1 F159V. Jun15702 can be used in studies related to enterovirus D68 (EV-D68) infection[1]. (Pink: Enterovirus ligand (HY-183010); Blue: Cereblon ligand (HY-183011); Black: linker).

IC50 & Target

Cereblon

 

体外研究
(In Vitro)

Jun15702 (10 μM; 0-8 h) 可在病毒进入前、进入过程中或进入后添加时，降低感染 EV-D68 US/MO/14−18947 的 RD 细胞中的 VP1 水平，并能有效降解耐普来可那立的 VP1F159V 突变蛋白[1]。
Jun15702 (0.3-30 μM; 2-10 h) 可在 EV-D68 US/MO/14-18947 感染的 RD 细胞中诱导 VP1 蛋白呈剂量依赖性、CRBN 介导的降解，该结果经蛋白质免疫印迹分析证实[1]。
Jun15702 对 RD 细胞的 CC50 为 81.8 μM (60 h)，在 50 μM 以下浓度时无显著细胞毒性[1]。

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

Jun15702 相关抗体:

Immunofluorescence[1]

Cell Line: EV-D68 US/MO/14-18947-infected RD cells, rMO-VP1 F159V EV-D68-infected RD cells
Concentration: 10 μM
Incubation Time: -1-8 h, 0-8 h, 1-8 h, 2-8 h, 3-8 h, 4-8 h, 5-8 h, 6-8 h, 7-8 h (relative to infection; wild-type testing); 2-8 hpi (mutant strain testing)
Result: Nearly completely depleted VP1 levels when added before or during viral entry (-1-8 h, 0-8 h).
Retained potent inhibitory activity when added post-entry (2-8 h, 3-8 h, 4-8 h, 5-8 hpi), only gradually losing activity at 6-8 h and 7-8 hpi.
Dramatically reduced VP1 immunofluorescence signals when added at 2-8 hpi to rMO-VP1 F159V-infected cells, whereas pleconaril showed no inhibition.

Western Blot Analysis[1]

Cell Line: EV-D68 US/MO/14-18947-infected RD cells
Concentration: 0, 0.3, 1, 3, 10, 30 μM; 10 μM lenalidomide-5-Br combined with increasing concentrations of Jun15702
Incubation Time: 2-10 hpi
Result: Caused a dose-dependent reduction in VP1 protein levels, whereas pleconaril and lenalidomide-5-Br did not induce VP1 degradation.
Preserved VP1 degradation at concentrations above 3 μM when combined with 10 μM lenalidomide-5-Br.
分子量

949.97

Formula

C47H54F3N7O11
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Jun15702 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Jun15702Jun 15702Jun-15702PROTACsEnterovirusRhinovirusHRVHRVsHEVHEVswild-type Enterovirus D68 strainsubiquitin-proteasome pathwayVP1rMO-VP1 F159VEnterovirus D68RD cellsEV-D68 US/MO/14?18947Cereblonpleconaril-resistant Enterovirus D68 variantCRBNInhibitorinhibitorinhibit

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