RN341
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.
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- CAS. Nr.: 3091508-57-2
- Formel: C30H34N8OS
- Molecular Weight:554.71
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
RN341 (Compound IRN341) (0.25-10 μM, 4 h) specifically inhibits substrate phosphorylation of LRRK1/2 but does not affect the biomarker site S935[1].
RN341 (1-10 μM) inhibits the residual activity of 10 kinases to less than 30 % at high concentrations, as shown in an activity screening of 350 kinases[1].
RN341 (0.01-10 μM) shows EC50 values indicating that, among the 12 identified off-target kinases, only 4 (STK10, MAPK14, JNK2, and TTK) are inhibited, with EC50s in the low micromolar range (<5 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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)
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Concentration:0.25 μM, 0.5 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:4 h
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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.
Chemical Information
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CAS. Nr. 3091508-57-2
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Molecular Weight 554.71
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Formel C30H34N8OS
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SMILES
O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=CC(C4=CNC5=NC(SCC)=NC(NC)=C54)=CC=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
RN341 Related Classifications
HY-174427 Related Classifications
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