2. PROTAC Neuronal Signaling
  3. PROTACs α-synuclein
  4. Arg-PEG1-Tαsyn

Arg-PEG1-Tαsyn 是一种靶向 α-syn的 PROTAC 降解剂，在 U251 细胞中其DC50 为 0.28  μM。Arg-PEG1-Tα-syn 采用氨基酸精氨酸 (Arg) 作为 E3 连接酶配体，并采用一种苯并噻唑-苯胺变体作为靶向 α-突触核蛋白 (α-syn) 的弹头。Arg-PEG1-Tαsyn 在哺乳动物细胞中对野生型α-突触核蛋白（α-syn）及其A53T突变体均表现出高效的降解效果。Arg-PEG1-Tαsyn 在体外通过 E3 泛素连接酶 UBR1 显著减少 α-syn 聚集。在体内，Arg-PEG1-Tαsyn 具有良好的安全性，并能显著改善多巴胺能神经元损伤和运动功能障碍。Arg-PEG1-Tαsyn 可用于帕金森病的相关研究。

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Arg-PEG1-Tαsyn

Arg-PEG1-Tαsyn Chemical Structure

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Arg-PEG1-Tαsyn 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Arg-PEG1-Tαsyn is an α-syn PROTAC degrader with a DC50 of 0.28 μM in U251 cells. Arg-PEG1-Tαsyn employs the amino acid arginine (Arg) as the E3 ligase UBR1 ligand and a benzothiazole-aniline variant as the warhead for α-syn. Arg-PEG1-Tαsyn significantly reduces α-syn aggregates and improves the dopaminergic neuronal impairment and the locomotion with safety profile in vivo.Arg-PEG1-Tαsyn shows the high degradation effect in mammalian cells for both wild-type α-syn and the α-syn (A53T) mutant. Arg-PEG1-Tαsyn can be used for Parkinson’s disease research[1][2].

体外研究
(In Vitro)

Arg-PEG1-Tα-syn (0-10 μM，48 小时) 在 U251 细胞中显著促进 α-synA53T 的减少，其DC50 为 0.28 μM，在 5 μM浓度下 Dmax 达到 90.5%[1]。
Arg-PEG1-Tα-syn (1 μM，0-72 小时) 在 U251/α-synA53T 细胞中随时间推移发挥 α-synA53T 降解作用[1]。
Arg-PEG1-Tα-syn (1 μM，48 小时) 在 U251/α-synWT、U251/α-synA53T、293/α-synWT、293/α-synA53T、SH-SY5Y/α-synWT 和 SH-SY5Y/α-synA53T 细胞中均表现出一致的 α-syn 降解效果[1]。
Arg-PEG1-Tα-syn 诱导的 α-synA53T 减少效应可被 MG132 (HY-13259) 逆转，但不被 Chloroquine (HY-17589A) 逆转[1]。
Arg-PEG1-Tα-syn (1 μM， 48 小时) 在 U251 细胞中通过 E3 泛素连接酶 UBR1 介导对 α-synWT 和 α-synA53T 的调控 (使用 shRNA 分别敲低了 UBR1, UBR2, UBR4 和 UBR5)[1]。
Arg-PEG1-Tα-syn (0-5 μM，48 小时) 通过减少 α-synA53T 聚集，在过表达 α-synWT 或 α-synA53T 的 SH-SY5Y 细胞中，保护细胞免受 α-syn WT 或 A53T 过表达诱导的毒性[1]。

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

Arg-PEG1-Tαsyn 相关抗体:

Western Blot Analysis[1]

Cell Line: U251/α-syn A53T cells
Concentration: 1 μM
Incubation Time: 0, 12, 24, 48 and 72 h
Result: Degraded the α-syn A53T as early as 12 h, reaching the peak at 48 h.

Western Blot Analysis[1]

Cell Line: U251/α-synWT, U251/α-synA53T, 293/α-synWT, 293/α-synA53T, SH-SY5Y/α-synWT and SH-SY5Y/α-synA53T cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Triggered efficient reduction of α-syn WT or α-syn A53T.

Western Blot Analysis[1]

Cell Line: U251 cells (knocked down UBR1, UBR2, UBR4, and UBR5 separately using shRNA)
Concentration: 1 μM
Incubation Time: 48 h
Result: Induced the degradation of both α-syn A53T and α-syn WT in U251 cells, an effect that is markedly suppressed by UBR1 knockdown but barely affected by UBR2, UBR4, or UBR5 knockdown.

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells (overexpressing α-syn WT or α-syn A53T)
Concentration: 0, 1 and 5 μM
Incubation Time: 48 h
Result: Significantly enhanced cell viability in α-syn WT cells at 5 μM and in α-syn A53T cells starting at 1 μM.

Immunofluorescence[1]

Cell Line: SH-SY5Y cells
Concentration: 5 μM
Incubation Time: 48 h
Result: Significantly reduced α-syn A53T aggregates.
Reduced α-syn A53T aggregates.
体内研究
(In Vivo)

Arg-PEG1-Tα-syn (不同浓度与 OP50 细菌混合，p.o.，从 L1 幼虫期持续处理至成虫第 5 天) 在秀丽隐杆线虫 NL5901 品系中能够减少 α-突触核蛋白聚集物，能显著改神经元胞体和突触的形态以及能部分恢复由 α-突触核蛋白病理引起的多巴胺能神经元功能缺陷[1]。
Arg-PEG1-Tα-syn (0-10 μM 浓度范围内与 OP50 细菌混合，p.o.，从 L1 幼虫期持续处理至成虫第 5 天) 能以剂量依赖的方式有效改善由 α-突触核蛋白病理引起的运动功能障碍，此效果在过表达人源 α-syn A53T 的线虫中得到证实，并在 UM0020 品系及野生型线虫中表现出良好的安全性[1]。

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

Animal Model: C. elegans UM0020 (A537 mutant) and C. elegans NL5901 (W.T.)[1]
Dosage: 0, 5 and 10 μM
Administration: p.o., om the L1 larval stage to day-5 adulthood
Result: Significantly rescued the locomotor deficits of UM0020 worms at day-1 and day-5 of adulthood, with a more pronounced effect at day-5.
Significantly improved the locomotor performance of UM0020 worms at 1 μM.
Animal Model: C. elegans UM0020 and C. elegans NL5901 (W.T.)[1]
Dosage: 5 μM
Administration: p.o., om the L1 larval stage to day-5 adulthood
Result: Has no significant difference in thrashing frequency.
分子量

455.58

Formula

C22H29N7O2S
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

Arg-PEG1-Tαsyn 相关分类

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Keywords:

Arg-PEG1-TαsynPROTACsα-synucleinα-SynU251 cellsUBR1dopaminergic neuronalParkinson’s diseaseInhibitorinhibitorinhibit

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