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LRRK2-IN-1
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C31H38N8O3
- MW: 570.69
Description
LRRK2-IN-1 is a potent ATP-competitive inhibitor of leucine-rich repeat kinase 2 (LRRK2), including the Parkinson's disease-associated G2019S mutant. It is widely used as a reference compound for LRRK2 kinase signaling studies.
LRRK2 regulates vesicle trafficking, autophagy, lysosomal function and neuroinflammatory signaling. LRRK2-IN-1 is valuable for pharmacological interrogation of LRRK2 activity, although experimental interpretation should consider off-target and permeability limitations reported for early LRRK2 inhibitors.
Key Features
- ATP-competitive LRRK2 kinase inhibitor
- Reported IC50 values: 13 nM for wild-type LRRK2 and 6 nM for G2019S LRRK2
- Reference tool for Parkinson's disease-related kinase biology
- Inhibits LRRK2 phosphorylation-dependent signaling
Applications
- LRRK2 kinase pharmacology
- Parkinson's disease pathway research
- Autophagy and lysosomal signaling studies
- Kinase inhibitor assay controls
More Information
| Parent CAS No. | 1234480-84-2 |
|---|---|
| Chemical Name | 2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenylamino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one |
| SMILES | N1(C)C2=CC=CC=C2C(=O)N(C)C2=CN=C(NC3=CC=C(C(N4CCC(N5CCN(C)CC5)CC4)=O)C=C3OC)N=C12 |
| MFCD | N.A. |
| InChi | InChI=1S/C31H38N8O3/c1-35-15-17-38(18-16-35)22-11-13-39(14-12-22)29(40)21-9-10-24(27(19-21)42-4)33-31-32-20-26-28(34-31)36(2)25-8-6-5-7-23(25)30(41)37(26)3/h5-10,19-20,22H,11-18H2,1-4H3,(H,32,33,34) |
| InChiKey | IWMCPJZTADUIFX-UHFFFAOYSA-N |
| CID | 46843906 |
| Short Description | LRRK2 inhibitor |
References
- B.K. Gilsbach et al. Structural Characterization of LRRK2 Inhibitors. J Med Chem. 2015 May 14;58(9):3751-6.
- X. Deng et al. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol. 2011 Apr;7(4):203-5.
- L. Munoz et al. Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation. Eur J Med Chem. 2015 May 5;95:29-34.
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