LRRK2-IN-1

Pricing Availability Delivery Time Qty
Cat.No. 4273 - LRRK2-IN-1 | C31H38N8O3 | CAS No. 1234480-84-2
Description: Potent and selective LRRK2 inhibitor
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)
Datasheet
Citations (3)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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Keywords: LRRK2-IN-1, supplier, parkinsons, disease, lrrk2, leucine-rich, repeat, kinase, 2, dardarin, parkinson's, LRRK2, LRRK2, Tocris Bioscience

3 Citations for LRRK2-IN-1

Citations are publications that use Tocris products. Selected citations for LRRK2-IN-1 include:

Reynolds et al (2014) LRRK2 kinase activity and biology are not uniformly predicted by its autophosphorylation and cellular phosphorylation site status. Front Mol Neurosci 7 54 PMID: 25009464

Saez-Atienzar et al (2014) The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. Cell Death Dis. 5 e1368 PMID: 25118928

Chia et al (2014) Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7. BMC Cancer 5 5827 PMID: 25500533


Do you know of a great paper that uses LRRK2-IN-1 from Tocris? If so please let us know.

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Literature in this Area

Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
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Parkinson's

Parkinson's Poster

Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.

Pathways for LRRK2-IN-1

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