Chemical Name: 5,11-Dihydro-2-[[2-methoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
Select another language:
View SDS
References
References are publications that support the products' biological activity.
Denget al (2011) Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat.Chem.Biol. 7 203 PMID: 21378983
Zhaoet al (2015) LRRK2 Dephosphorylation increases its ubiquitination. Biochem.J. 469 107 PMID: 25939886