LRRK2-IN-1

Catalog No.S7584

LRRK2-IN-1 Chemical Structure

Molecular Weight(MW): 570.69

LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.

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Biological Activity

Description LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
Targets
LRRK2 (G2019S) [1]
(Cell-free assay)
LRRK2 (WT) [1]
(Cell-free assay)
DCLK2 [1]
(Cell-free assay)
6 nM 13 nM 45 nM
In vitro

In HEK 293 cells stably expressing GFP-LRRK2[G2019S], LRRK2-IN-1 alters the cytoplasmic localization of LRRK2. In human-derived neuroblastoma SHSY5Y cells and mouse Swiss 3T3 cells, LRRK2-IN-1 induces a similar dose-dependent Ser910 and Ser935 dephosphorylation and loss of 14-3-3 binding to endogenous LRRK2. [1] In transgenic C. elegans expressing human R1441C- and G2019S-LRRK2, LRRK2-IN1 rescues the behavioral deficit characteristic of dopaminergic impairment. [2] In mouse fibroblasts, LRRK2-IN1 reduces cell motility. [3] In AsPC-1 and HCT116 cell lines, LRRK2-IN-1 shows anti-proliferative and pro-apoptotic properties, induces G1 and G2/M cell cycle arrest and inhibits DCLK1 mRNA and protein expression. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells MlTTSpVv[3Srb36gZZN{[Xl? Mn;aTY5pcWKrdHnvckBw\iCOUmLLNkBIOjBzOWOgcZV1[W62IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNidYPpcochdmmldHnk[UBidmRiQWTQJIF{KHO3YoP0doF1\SxiSVO1NF0xNjByNjFOwG0> NFLMR20zOjN|NUi5Oy=>
HEK293 cells M4\wNGZ2dmO2aX;uJIF{e2G7 NXHlXWJZOC5yMz2zJO69VQ>? Mm\iPVAhdWmwcx?= M{jPe2lvcGmkaYTpc44hd2Zid3ns[E11gXCnIFzSVmszKHCqb4PwbI9zgWyjdHnvckBifCCVZYK5N|Uh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{BifCByLkCzJJRwKDNidV2gZYZ1\XJiOUCgcYlveyCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz NGLifZUzOjN|NUi5Oy=>
lymphoblastoid cells NWrIZ4ZNTnWwY4Tpc44h[XO|YYm= NFTIcGsxNjB|IITvJFMhfU1? Mo\pPVAhdWmwcx?= NF63OnRKdmirYnn0bY9vKG:oIFzSVmszKGmwIHj1cYFvKGy7bYDoc4Jt[XO2b3nkJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiU3XyPVExKGG3dH;wbI9{eGixconsZZRqd25iYYSgNE4xOyC2bzCzJJVOKGGodHXyJFkxKG2rboOgZpkhcW2vdX7vZoxwfCCvZYToc4Q> NUPhcHNjOjJ6NkOyNFM>

... Click to View More Cell Line Experimental Data

In vivo In wild type male C57BL/6 mice, LRRK2-IN-1 (100 mg/kg, i.p.) inhibits Ser910 and Ser935 dephosphorylation of LRRK2 in the kidney, while no effects in the brain. [1]

Protocol

Kinase Assay:[1]
+ Expand

IC50 determination:

Active GST-LRRK2 (1326-2527), GST-LRRK2 [G2019S] (1326-2527), GST-LRRK2 [A2016T] (1326-2527) and GST-LRRK2 [A2016T+G2019S] (1326-2527) enzyme is purified with glutathione sepharose from HEK293 cell lysate 36 h following transient transfection of the appropriate cDNA constructs. Peptide kinase assays, performed in duplicate, are set up in a total volume of 40 µL containing 0.5 µg LRRK2 kinase (which at approximately 10% purity gives a final concentration of 8 nM) in 50 mM Tris/HCl, pH 7.5, 0.1 mM EGTA, 10 mM MgCl2, 20 µM Nictide, 0.1 µM [γ-32P]ATP (~500 cpm/pmol) and the indicated concentrations of inhibitor dissolved in DMSO. After incubation for 15 min at 30 °C, reactions are terminated by spotting 35 µL of the reaction mix onto P81 phosphocellulose paper and immersion in 50 mM phosphoric acid. Samples are washed extensively and the incorporation of [γ-32P]ATP into Nictide is quantified by Cerenkov counting. IC50 values are calculated with GraphPad Prism using non-linear regression analysis.
Cell Research:[4]
+ Expand
  • Cell lines: HCT116, and AsPC-1 cells
  • Concentrations: 20 μM
  • Incubation Time: 48 h
  • Method: Cells are seeded into a 96-well tissue culture plate in triplicate. The cells are cultured in the presence of LRRK2-IN-1 with DMSO as a vehicle at 0, 0.31, 0.63, 1, 2, and 5, 10, and 20 μM. 48 h post treatment, 10 μL of TACS MTT Reagent (RND Systems) is added to each well and the cells are incubated at 37°C until dark crystalline precipitate became visible in the cells. 100 μL of 266 mM NH4OH in DMSO is then added to the wells and placed on a plate shaker at low speed for 1 minute. After shaking, the plate is allowed to incubate for 10 minutes protected from light and the OD550 for each well is read using a microplate reader. The results are averaged and calculated as a percentage of the DMSO (vehicle) control +/- the standard error of the mean.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Wild type male C57BL/6 mice
  • Formulation: Captisol
  • Dosages: 100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (175.22 mM)
Ethanol 100 mg/mL (175.22 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Captisol
For best results, use promptly after mixing.
17mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 570.69
Formula

C31H38N8O3

CAS No. 1234480-84-2
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID