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LRRK2-IN-1

Catalog No. T2246 CAS 1234480-84-2

LRRK2-IN-1 is an effective and selective LRRK2 inhibitor.

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LRRK2-IN-1, CAS 1234480-84-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 60.00
10 mg	In stock	$ 86.00
25 mg	In stock	$ 177.00
50 mg	In stock	$ 321.00
100 mg	In stock	$ 563.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 98.44%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LRRK2-IN-1 is an effective and selective LRRK2 inhibitor.
Targets&IC50	LRRK2 (WT):13 nM, DCLK2:45 nM, LRRK2 (G2019S):6 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]
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]
Kinase Assay	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	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)

Molecular Weight	570.69
Formula	C31H38N8O3
CAS No.	1234480-84-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 57 mg/mL (100 mM)

DMSO: 57 mg/mL (100 mM)

References and Literature

1. Deng X, et al. Nat Chem Biol. 2011, 7(4), 203-205. 2. Yao C, et al. Hum Mol Genet. 2013, 22(2), 328-344. 3. Caesar M, et al. Neurobiol Dis. 2013, 54, 280-288. 4. Weygant N, et al. Mol Cancer. 2014, 13, 103. 5. Yan R, Li J J, Zhou Y, et al. Inhibition of DCLK1 down-regulates PD-L1 expression through Hippo pathway in human pancreatic cancer[J]. Life Sciences. 2020, 241: 117150.

Citations

1. Yan R, Li J J, Zhou Y, et al. Inhibition of DCLK1 down-regulates PD-L1 expression through Hippo pathway in human pancreatic cancer. Life Sciences. 2020, 241: 117150 2. Wan J, He Z, Peng R, et al.Injectable photocrosslinking spherical hydrogel-encapsulated targeting peptide-modified engineered exosomes for osteoarthritis therapy.Journal of Nanobiotechnology.2023, 21(1): 1-21.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Kinase Inhibitor Library Cell Cycle Compound Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Aging Compound Library Autophagy Compound Library NO PAINS Compound Library Apoptosis Compound Library

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Keywords

LRRK2-IN-1 1234480-84-2 Apoptosis Autophagy Cell Cycle/Checkpoint LRRK2 CDK Leucine-rich repeat kinase 2 Inhibitor LRRK2 IN 1 LRRK2IN1 inhibit LRRK-2-IN-1 inhibitor

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