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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 3091508-57-2
- 화학식: C30H34N8OS
- 분자량:554.71
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
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.
-
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.
Chemical Information
-
CAS No. 3091508-57-2
-
분자량 554.71
-
화학식 C30H34N8OS
-
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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RN341 Related Classifications
HY-174427 Related Classifications
Powered by Bioz