Biological Activity
Potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2). Inhibits both G2019S mutant and wild-type LRRK2 kinase activity (IC50 values are 6 and 13 nM respectively). Causes dephosphorylation, ubiquitination and degradation of LRRK2.
Licensing Information
Sold under license from the Dana-Farber Cancer Institute.
Compound Libraries
LRRK2-IN-1 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 570.09 |
| Formula | C31H38N8O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1234480-84-2 |
| PubChem ID | 46843906 |
| InChI Key | IWMCPJZTADUIFX-UHFFFAOYSA-N |
| Smiles | O=C2C3=C(C=CC=C3)N(C)C1=NC(NC4=C(OC)C=C(C(N5CCC(N6CCN(C)CC6)CC5)=O)C=C4)=NC=C1N2C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.01 | 100 | |
| ethanol | 57.01 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 570.09. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.75 mL | 8.77 mL | 17.54 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.51 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.75 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Deng et al (2011) Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat.Chem.Biol. 7 203 PMID: 21378983
Zhao et al (2015) LRRK2 Dephosphorylation increases its ubiquitination. Biochem.J. 469 107 PMID: 25939886
Keywords: LRRK2-IN-1, supplier, parkinsons, disease, lrrk2, leucine-rich, repeat, kinase, 2, dardarin, parkinson's, LRRK2, LRRK2, Tocris Bioscience
