LRRK2-IN-1
Based on 8 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.04%
- CAS No.: 1234480-84-2
- Formule: C31H38N8O3
- Masse moléculaire:570.69
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) LRRK2-IN-1
More- Nat Commun. 2026 Feb 28;17(1):3324. [Abstract]
- Cells. 2024 Mar 23;13(7):565. [Abstract]
- Mol Pharm. 2018 Aug 6;15(8):3252-3259. [Abstract]
- Exp Neurol. 2026 Oct:404:115873. [Abstract]
- iScience. 2023 Oct 5;26(11):108130. [Abstract]
- Anticancer Res. 2018 Nov;38(11):6225-6230. [Abstract]
- bioRxiv. 2023 Jun 30:2023.06.28.546897. [Abstract]
- Harvard Medical School LINCS LIBRARY
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Activité biologique
IC50: 13 nM (WT), 6 nM (G2019S)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
13 nM
Compound: LRRK2IN1
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Inhibition of wild-type GST-tagged LRRK2 (1326 to 2527 aa)(unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method
Inhibition of wild-type GST-tagged LRRK2 (1326 to 2527 aa)(unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method
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[PMID: 25791676] |
| HEK293 | IC50 |
13 nM
Compound: LRRK2-IN-1
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Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate
Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate
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[PMID: 22335897] |
| HEK293 | IC50 |
2450 nM
Compound: LRRK2-IN-1
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Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate
Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate
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[PMID: 22335897] |
| HEK293 | IC50 |
3080 nM
Compound: LRRK2-IN-1
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Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate
Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate
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[PMID: 22335897] |
| HEK293 | IC50 |
6 nM
Compound: LRRK2-IN-1
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Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate
Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate
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[PMID: 22335897] |
| HEK293 | IC50 |
7.9 nM
Compound: LRRK2IN1
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Inhibition of LRRK2 G2019S mutant (1326 to 252 aa) (unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method
Inhibition of LRRK2 G2019S mutant (1326 to 252 aa) (unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method
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[PMID: 25791676] |
| HEK-293T | IC50 |
2800 nM
Compound: LRRK2-IN-1
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Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
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[PMID: 34710325] |
| MM1.S | IC50 |
530 nM
Compound: LRRK2-IN-1
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Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
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[PMID: 34710325] |
| U-87MG ATCC | EC50 |
0.66 μM
Compound: LRRK2IN1
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Inhibition of IL6 secretion in LPS/IL-1beta-stimulated human U87 cells compound pretreated for 30 mins before stimulation measured after 24 hrs by ELISA
Inhibition of IL6 secretion in LPS/IL-1beta-stimulated human U87 cells compound pretreated for 30 mins before stimulation measured after 24 hrs by ELISA
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[PMID: 25791676] |
Wild-type and G2019S transduction results in 2.5 fold higher TR-FRET signal which can be inhibited by LRRK2-IN-1 in a dose-dependent manner with IC50 values of 0.08 μM and 0.03 μM, respectively[1]. LRRK2-IN-1 possessed an IC50 of 45 nM for inhibition of DCLK2 and exhibits an IC50 of greater than 1 μM when evaluated in biochemical assays for AURKB, CHEK2, MKNK2, MYLK, NUAK1, and PLK1. LRRK2-IN-1 is confirmed to inhibit MAPK7 with an EC50 of 160 nM. LRRK2-IN-1 induces a dose dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells[2]. LRRK2-IN-1 is moderately cytotoxic with IC50 of 49.3 μM in HepG2 cells. LRRK2-IN-1 exhibits genotoxicity in the presence and absence of S9 at 15.6 and 3.9 μM, respectively[3]. LRRK2-IN-1 inhibits proliferation, migration, and induces cell death with hallmarks of apoptosis of HCT116 and AsPC-1 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1234480-84-2
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Appearance Solid
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Masse moléculaire 570.69
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Formule C31H38N8O3
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Color Light yellow to yellow
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SMILES
O=C(C1=CC(OC)=C(NC2=NC=C3C(N(C4=C(C(N3C)=O)C=CC=C4)C)=N2)C=C1)N5CCC(CC5)N6CCN(CC6)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Commun
Targeting leucine-rich repeat kinase 2 overcomes resistance to oncolytic herpes simplex virus-based therapies in glioblastoma. [Abstract]2026 Feb 28;17(1):3324. PMID: 41764166 -
Cells
LRRK2 G2019S Promotes Colon Cancer Potentially via LRRK2-GSDMD Axis-Mediated Gut Inflammation. [Abstract]2024 Mar 23;13(7):565. PMID: 38607004 -
Mol Pharm
Chemoproteomics Reveals the Antiproliferative Potential of Parkinson's Disease Kinase Inhibitor LRRK2-IN-1 by Targeting PCNA Protein. [Abstract]2018 Aug 6;15(8):3252-3259. PMID: 29993254
LRRK2-IN-1 purchased from MedChemExpress. Usage Cited in: Mol Pharm. 2018 Aug 6;15(8):3252-3259. [Abstract]
Western blot analysis the expression of c-Myc and DCLK1 treated with or without LRRK2-IN-1 in Jurkat cells.
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Exp Neurol
Systemic characterization of aging-related phenotypes induced by wild-type and G2019S LRRK2 in Caenorhabditis elegans. [Abstract]2026 Oct:404:115873. PMID: 42270006 -
iScience
LRRK2 G2019S promotes astrocytic inflammation induced by oligomeric α-synuclein through NF-κB pathway. [Abstract]2023 Oct 5;26(11):108130. PMID: 37876795 -
Anticancer Res
Dclk1 Inhibition Cancels 5-FU-induced Cell-cycle Arrest and Decreases Cell Survival in Colorectal Cancer. [Abstract]2018 Nov;38(11):6225-6230. PMID: 30396941
LRRK2-IN-1 purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2018 Nov;38(11):6225-6230. [Abstract]
Effect of 5-FU, LRRK, or 5-FU and LRRK combined treatment on Chk1 phosphorylation.
LRRK2-IN-1 purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2018 Nov;38(11):6225-6230. [Abstract]
Effect of 5-FU, LRRK treatment, or combined treatment with 5-FU and LRRK on PARP-1 cleavage.
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bioRxiv
LRRK2 G2019S promotes the development of colon cancer via modulating intestinal inflammation. [Abstract]2023 Jun 30:2023.06.28.546897. PMID: 37425755 -
Harvard Medical School LINCS LIBRARY
Solvant et solubilité
DMSO : 30 mg/mL (52.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells (104 cells per well) 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 is added to each well and the cells are incubated at 37°C until dark crystalline precipitate become 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LRRK2-IN-1 is dissolved in Captisol and administered by intraperitoneal injection into wild type male C57BL/6 mice at a dose of 100 mg/kg. Control mice are injected with an equal volume of Captisol. At 1 and 2 h time points, mice are extinguwashed by cervical dislocation and kidney and brain tissue rapidly dissected and snap-frozen in liquid nitrogen.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Hermanson SB, et al. Screening for Novel LRRK2 Inhibitors Using a High-Throughput TR-FRET Cellular Assay for LRRK2 Ser935 Phosphorylation.PLoS One. 2012;7(8):e43580. Epub 2012 Aug 28. [Content Brief]
[3]. Koshibu K, et al. Alternative to LRRK2-IN-1 for Pharmacological Studies of Parkinson's Disease. Pharmacology. 2015;96(5-6):240-7. [Content Brief]
[4]. Weygant N, et al. Small molecule kinase inhibitor LRRK2-IN-1 demonstrates potent activity against colorectal and pancreatic cancer through inhibition of doublecortin-like kinase 1. Mol Cancer. 2014 May 6;13:103. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7523 mL | 8.7613 mL | 17.5226 mL | 43.8066 mL |
| 5 mM | 0.3505 mL | 1.7523 mL | 3.5045 mL | 8.7613 mL | |
| 10 mM | 0.1752 mL | 0.8761 mL | 1.7523 mL | 4.3807 mL | |
| 15 mM | 0.1168 mL | 0.5841 mL | 1.1682 mL | 2.9204 mL | |
| 20 mM | 0.0876 mL | 0.4381 mL | 0.8761 mL | 2.1903 mL | |
| 25 mM | 0.0701 mL | 0.3505 mL | 0.7009 mL | 1.7523 mL | |
| 30 mM | 0.0584 mL | 0.2920 mL | 0.5841 mL | 1.4602 mL | |
| 40 mM | 0.0438 mL | 0.2190 mL | 0.4381 mL | 1.0952 mL | |
| 50 mM | 0.0350 mL | 0.1752 mL | 0.3505 mL | 0.8761 mL |
LRRK2-IN-1 Related Classifications
HY-10875 Related Classifications
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