2. Autophagy
  3. LRRK2
  4. RN341

RN341 是 LRRK2 特异性 II 型激酶抑制剂 (IC50为 296 nM)。RN341 抑制 LRRK2 磷酸化，通过稳定开放构象避免 S935 去磷酸化。RN341 通过阻止微管结合挽救 LRRK2 介导的驱动蛋白运动阻滞。RN341 在细胞水平有效抑制 LRRK2 野生型及 G2019S 突变体。RN341 为帕金森病的研究提供了新方向[1]。

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RN341 Chemical Structure

RN341 Chemical Structure

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RN341 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RN341 is a specific type II kinase inhibitor of LRRK2 (IC50: 296 nM). RN341 inhibits LRRK2 phosphorylation and avoids S935 dephosphorylation by stabilizing the open conformation. RN341 rescues LRRK2-mediated kinesin motility block by preventing microtubule binding. RN341 effectively inhibits LRRK2 wild-type and G2019S mutant at the cellular level. RN341 provides a new direction for Parkinson's disease research[1].

体外研究
(In Vitro)

RN341 (Compound IRN341) (0.25-10 μM, 4 h) 特异性抑制 LRRK1/2 的底物磷酸化，但不影响生物标志物位点 S935[1]。
RN341 (1-10 μM) 在 350 种激酶的活性筛选中显示，在高浓度下可将 10 种激酶的残余活性抑制至 30 % 以下[1]。
RN341 (0.01-10 μM) 的 EC50 值表明，在已鉴定出的 12 种脱靶激酶中，只有 4 种 (STK10、MAPK14、JNK2 和 TTK)受到抑制，其 EC50 值处于低微摩尔范围 (<5 μM)[1]。

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

RN341 相关抗体:

Cell Viability Assay[1]

Cell Line: 293T cells (transfected with LRRK1 and its substrate Rab7), 293T cells (co-transfected with LRRK2 and GFP-Rab8a), 293T cells (transfected with GFP-Rab8a and either wild-type or G2019S LRRK2), 293T cells (transiently co-transfected with LRRK1 and its substrate GFP-Rab7), 293T cells (transiently co-transfected with GFP-Rab8a and either GFP-11 tagged wild-type (WT) or GFP-11 tagged G2019S LRRK2)
Concentration: 0.25 μM, 0.5 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 4 h
Result: Showed strong inhibitory effects on LRRK1 kinase activity, which in turn inhibited Rab7 S72 phosphorylation.
Inhibited LRRK2-mediated Rab8a phosphorylation in a dose-dependent manner.
Did not reduce LRRK2 biomarker site S935 phosphorylation.
分子量

554.71

Formula

C30H34N8OS
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

RN341 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

RN341RN 341RN-341LRRK2Leucine-rich repeat kinase 2293T cellsLRRK1/2Parkinson’s diseaseInhibitorinhibitorinhibit

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