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Cat. No.: HY-180320

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Lu AF58786

Lu AF58786 is a potent and selective LRRK2 inhibitor with an IC₅₀ of 12 nM. Lu AF58786 also exhibits inhibition activity against LRRK2 G2019S and LRRK2 A2016T with IC₅₀s of 19 and 93 nM. Lu AF58786 inhibits phosphorylation of LRRK2, Rab10 and Rab12 in human peripheral blood mononuclear cells. Lu AF58786 can be used for parkinson’s disease research.

For research use only. We do not sell to patients.

CAS No.: 1632368-13-8
Formula: C₁₉H₁₆N₆
Molecular Weight:328.37

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

Lu AF58786 Chemical Structure

CAS No.: 1632368-13-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

LRRK2 G2019S

19 nM (IC₅₀)

LRRK2 A2016T

93 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	17 nM Compound: 23	Inhibition of human wild type LRRK2 phosphorylation at ser935 expressed in BacMam transduced HEK293 cells after 48 hrs by in-cell Western assay Inhibition of human wild type LRRK2 phosphorylation at ser935 expressed in BacMam transduced HEK293 cells after 48 hrs by in-cell Western assay	[PMID: 29023112]

Chemical Information

CAS No. 1632368-13-8
Molecular Weight 328.37
Formula C₁₉H₁₆N₆
SMILES

N#CC1=CNC2=NC(NC3=NN(C)C=C3)=CC(C4=CC(C)=CC=C4)=C12
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Thirstrup K, et al. Selective LRRK2 kinase inhibition reduces phosphorylation of endogenous Rab10 and Rab12 in human peripheral mononuclear blood cells. Sci Rep. 2017 Aug 31;7(1):10300. [Content Brief]

[2]. Williamson DS, et al. Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1). J Med Chem. 2017 Nov 9;60(21):8945-8962. [Content Brief]

Calculators

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Dilution Calculator

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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