2. Autophagy MAPK/ERK Pathway
  3. LRRK2 MNK
  4. HG-10-102-01

HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research.

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

HG-10-102-01 Chemical Structure

HG-10-102-01 Chemical Structure

CAS No. : 1351758-81-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
1 mg USD 37 In-stock
5 mg USD 110 In-stock
10 mg USD 175 In-stock
25 mg USD 350 In-stock
50 mg USD 560 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

HG-10-102-01 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE HG-10-102-01

View All MNK Isoform Specific Products:

View All Isoforms
MNK1 MNK2 MNK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research[1][2].

IC50 & Target

IC50: 3.2 nM (LRRK2[G2019S]), 20.3 nM (wild-type LRRK2), 95.9 nM (LRRK2[G2019S+A2016T], 153.7 nM (LRRK2[A2016T]), 0.6 μM (MNK2), 2.1 μM (MLK1)[1]
In Vitro

HG-10-102-01 (0-3 μM, 90 min) substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HG-10-102-01 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293 cells, Mouse Swiss 3T3 cells and Mouse embryonic fibroblast cells
Concentration: 0, 0.01, 0.03, 0.1, 0.3, 1, and 3 μM
Incubation Time: 90 min
Result: Induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells. Induced similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells and mouse embryonic fibroblast cells.
In Vivo

HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice[1].
HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wild type male C57BL/6 mice[1]
Dosage: 0, 3, 10, 30, 50, and 100 mg/kg
Administration: IP, once
Result: Showed near complete dephosphorylation of Ser910 and Ser935 of LRRK2 in all tissues including brain at 100 mg/kg and 50 mg/kg, but only partial inhibition in brain at the 30 and 10 mg/kg doses.
Animal Model: Wild type male C57BL/6 mice[1]
Dosage: 1 mg/kg (IV); 10 mg/kg (PO)
Administration: IV, PO; once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of HG-10-102-01 in male C57BL/6 mice[1].
IV (1 mg/kg) PO (10 mg/kg)
Tmax (h) 0.25
Cmax (ng/mL) 1330 1241
AUClast (ng/mL∗h) 74.85 502.34
AUCINF (ng/mL∗h) 75.06 503.41
T1/2 (h) 0.13
CL (mL/min/kg) 222.04
Vss (L/kg) 1.68
F (%) 67
Molecular Weight

377.83

Formula

C17H20ClN5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(C(N2CCOCC2)=O)=CC=C1NC3=NC(NC)=C(Cl)C=N3
Shipping

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

DMSO : ≥ 50 mg/mL (132.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6467 mL 13.2335 mL 26.4669 mL
5 mM 0.5293 mL 2.6467 mL 5.2934 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (5.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (5.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6467 mL 13.2335 mL 26.4669 mL 66.1673 mL
5 mM 0.5293 mL 2.6467 mL 5.2934 mL 13.2335 mL
10 mM 0.2647 mL 1.3233 mL 2.6467 mL 6.6167 mL
15 mM 0.1764 mL 0.8822 mL 1.7645 mL 4.4112 mL
20 mM 0.1323 mL 0.6617 mL 1.3233 mL 3.3084 mL
25 mM 0.1059 mL 0.5293 mL 1.0587 mL 2.6467 mL
30 mM 0.0882 mL 0.4411 mL 0.8822 mL 2.2056 mL
40 mM 0.0662 mL 0.3308 mL 0.6617 mL 1.6542 mL
50 mM 0.0529 mL 0.2647 mL 0.5293 mL 1.3233 mL
60 mM 0.0441 mL 0.2206 mL 0.4411 mL 1.1028 mL
80 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8271 mL
100 mM 0.0265 mL 0.1323 mL 0.2647 mL 0.6617 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

HG-10-102-01 Related Classifications

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.

Keywords:

HG-10-102-011351758-81-0LRRK2MNKLeucine-rich repeat kinase 2Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseRadiosynthesisPositron emission tomographyPETParkinson’s diseaseBBBHEK293 cellsMouse Swiss 3T3 cellsMouse embryonic fibroblast cellsSer910Ser935Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
HG-10-102-01
Cat. No.:
HY-13488
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.