2. Autophagy
    Apoptosis
  3. LRRK2
    Apoptosis
  4. LRRK2-IN-1

LRRK2-IN-1 

Cat. No.: HY-10875 Purity: 99.12%
COA Handling Instructions

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.

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

LRRK2-IN-1 Chemical Structure

LRRK2-IN-1 Chemical Structure

CAS No. : 1234480-84-2

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 132 In-stock
Solid
10 mg USD 121 In-stock
50 mg USD 440 In-stock
100 mg USD 770 In-stock
500 mg USD 1815 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    LRRK2-IN-1 purchased from MCE. 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.

    LRRK2-IN-1 purchased from MCE. 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 MCE. 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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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.

    IC50 & Target

    IC50: 13 nM (WT), 6 nM (G2019S)
    In Vitro

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    LRRK2-IN-1 (100 mg/kg, i.p.) induces dephosphorylation of LRRK2 in the kidney of the mice[2]. Peritumoral injection of LRRK2-IN-1 (100 mg/kg) results in a significant decrease in tumor volume and weight of AsPC-1 tumor xenografts[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    570.69

    Appearance

    Solid

    Formula

    C31H38N8O3
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 30 mg/mL (52.57 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7523 mL 8.7613 mL 17.5226 mL
    5 mM 0.3505 mL 1.7523 mL 3.5045 mL
    10 mM 0.1752 mL 0.8761 mL 1.7523 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

      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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.12%

    COA (251 KB) HNMR (127 KB) RP-HPLC (140 KB) LCMS (296 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [4]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    LRRK2-IN-11234480-84-2LRRK2ApoptosisLeucine-rich repeat kinase 2Inhibitorinhibitorinhibit

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