Cat. No.: HY-111493

LRRK2 inhibitor 1

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Based on 1 Customer Validation

LRRK2 inhibitor 1 is a LRRK2 inhibitor. LRRK2 inhibitor 1 blocks STAT1 phosphorylation and the expression of interferon-stimulated genes, and inhibits intracellular innate immune responses. LRRK2 inhibitor 1 enhances oncolytic virus infection, replication and viral protein expression in tumor cells, promotes tumor cell apoptosis, and cooperates with oncolytic viruses to reduce tumor cell viability. LRRK2 inhibitor 1 enhances the oncolytic activity of multiple oncolytic viruses, and inhibits the growth of glioma xenografts when used in combination with oncolytic viruses. LRRK2 inhibitor 1 can be used in research related to various cancers such as lung cancer, colorectal cancer and liver cancer.

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

Purity: 99.80%
CAS No.: 1802525-61-6
Formula: C₂₀H₂₃N₅O₄
Molecular Weight:397.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LRRK2 inhibitor 1 Chemical Structure

CAS No.: 1802525-61-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

STAT1

All STAT Isoforms :

In Vitro

LRRK2 inhibitor 1 (1-10 μM; 48 h) significantly enhances the killing effect of oHSV-GFP virus on various human cancer cell lines, including human lung cancer cell line A549 and human colorectal cancer cell line HT-29, and reduces cell viability^[1].
LRRK2 inhibitor 1 (5 μM) significantly promotes the replication of oHSV-GFP virus in human glioblastoma cell lines U-251MG, U-87MG, U-118MG and GBM, enhances viral protein expression, and improves viral infectivity^[1].
Combined treatment with LRRK2 inhibitor 1 (2.5 μM; 48 h) and oHSV-GFP virus significantly reduces the viability of human glioblastoma cell lines U-251MG and LN-18^[1].
LRRK2 inhibitor 1 (2.5 μM; 48 h) significantly enhances the killing effect of HSV-1 recombinant viruses D34.5, OVH, HSV-2 virus and adenovirus HADV5 on the human glioblastoma cell line U-251MG, and reduces cell viability^[1].
LRRK2 inhibitor 1 (5 μM; 12 h) enhances the infectivity of oHSV-GFP in the human glioblastoma cell line U-87MG by inhibiting phosphorylation of the STAT pathway and ISG gene expression, thereby suppressing intracellular innate immune responses^[1].
Combination treatment with LRRK2 inhibitor 1 (5 μM; 48 h) and oHSV-GFP virus significantly promotes early and late apoptosis in human glioblastoma cell lines U-251MG and U-118MG, thereby enhancing anti-tumor activity^[1].

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

Cell Viability Assay^[1]

Cell Line:

A549、HT-29、Hep G2、MDA-MB-231、HeLa、SK-OV-3、A-375、HEp-2、U-20S、Panc 10.5、FaDu、AGS、A-498
Concentration:

10 μM、5 μM、2 μM、1 μM
Incubation Time:

4 h (pre-incubation); 48 h (total treatment)
Result:

Reduced A549 cell viability from 98.1% to 64.59%.
Reduced A-498 cell viability from 85.6% to 72.8%.
Reduced HT-29 cell viability from 91.0% to 38.3%.
Reduced Hep G2 cell viability from 58.9% to 18.1%.
Reduced MDA-MB-231 cell viability from 81.4% to 26.0%.
Reduced HeLa cell viability from 63.8% to 14.5%.
Reduced SK-OV-3 cell viability from 98.6% to 64.3%.
Reduced A-375 cell viability from 100.1% to 19.9%.
Reduced HEp-2 cell viability from 98.0% to 68.0%.
Reduced U-20S cell viability from 97.3% to 78.8%.
Reduced Panc 10.5 cell viability from 91.8% to 61.3%.
Reduced FaDu cell viability from 95.1% to 22.3%.
Reduced AGS cell viability from 100.1% to 24.2%.

Cell Viability Assay^[1]

Cell Line:

U-251MG、LN-18
Concentration:

2.5 μM
Incubation Time:

4 h (pre-incubation); 48 h (total treatment)
Result:

Reduced cell viability significantly compared to virus-only group.
Achieved IC₅₀ shift of 10.42-fold in U-251MG cells.
Achieved IC₅₀ shift of 11.73-fold in LN-18 cells.

Apoptosis Analysis^[1]

Cell Line:

U-251MG、U-118MG
Concentration:

5 μM
Incubation Time:

4 h (pre-incubation); 48 h (total treatment)
Result:

Increased early apoptosis rate of U-251MG cells from 32.1% to 59.5%.
Increased late apoptosis rate of U-251MG cells from 19.9% to 25.6%.
Increased early apoptosis rate of U-118MG cells from 6.0% to 41.6%.
Increased late apoptosis rate of U-118MG cells from 9.0% to 15.6%.

Cell Viability Assay^[1]

Cell Line:

U-251MG
Concentration:

2.5 μM
Incubation Time:

4 h (pre-incubation); 48 h (total treatment)
Result:

Reduced U-251MG cell viability from 96.4% to 33.1% when combined with HSV-1 recombinant virus D34.5.
Reduced U-251MG cell viability from 107.0% to 20.1% when combined with HSV-1 recombinant virus OVH.
Reduced U-251MG cell viability from 66.1% to 32.3% when combined with HSV-2 virus.
Reduced U-251MG cell viability from 87.8% to 57.2% when combined with adenovirus HADV5.

In Vivo

LRRK2 inhibitor 1 (2 mg/kg; i.p.; once daily) combined with oHSV-GFP significantly inhibits the growth of human glioma U-87MG xenografts, with no significant effect on body weight and favorable safety profile^[1].
LRRK2 inhibitor 1 (2 mg/kg; i.p.; once daily) combined with oHSV-GFP significantly inhibits the growth of xenografts derived from the human glioma PDX model GBM-1, with no significant impact on body weight and favorable safety profile^[1].

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

Animal Model:

Nod Scid (6-week-old female)^[1]
Dosage:

2 mg/kg (LRRK2-IN-1); 1×10⁷ PFU/次 (oHSV-GFP)
Administration:

i.p. (daily); i.t. (every 2 days, 6 times total)
Result:

Did not reduce tumor volume compared with control group.
Significantly reduced tumor volume when combined with oHSV-GFP, with no significant effect on mouse body weight and good safety.

Animal Model:

Nod Scid (6-week-old female)^[1]
Dosage:

2 mg/kg (LRRK2-IN-1); 1×10⁷ PFU/次 (oHSV-GFP)
Administration:

i.p. (daily); i.t. (every 2 days, 3 times total)
Result:

Caused only slight tumor volume reduction compared with control group.
Significantly reduced tumor volume when combined with oHSV-GFP, with no significant effect on mouse body weight and good safety.

Chemical Information

CAS No. 1802525-61-6
Appearance Solid
Molecular Weight 397.43
Formula C₂₀H₂₃N₅O₄
Color White to off-white
SMILES

CCOC1=NC(NC2=C(OC)C=C(C(N3CCOCC3)=O)C=C2)=NC4=C1C=CN4
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 : 62.5 mg/mL (157.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5162 mL

12.5808 mL

25.1617 mL

5 mM

0.5032 mL

2.5162 mL

5.0323 mL

10 mM

0.2516 mL

1.2581 mL

2.5162 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (5.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: 2.08 mg/mL (5.23 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Huang Chenghao, et al. Application of LRRK2 inhibitors in anti-tumor. CN118526597A. 2024-08-23.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.5162 mL	12.5808 mL	25.1617 mL	62.9042 mL
	5 mM	0.5032 mL	2.5162 mL	5.0323 mL	12.5808 mL
	10 mM	0.2516 mL	1.2581 mL	2.5162 mL	6.2904 mL
	15 mM	0.1677 mL	0.8387 mL	1.6774 mL	4.1936 mL
	20 mM	0.1258 mL	0.6290 mL	1.2581 mL	3.1452 mL
	25 mM	0.1006 mL	0.5032 mL	1.0065 mL	2.5162 mL
	30 mM	0.0839 mL	0.4194 mL	0.8387 mL	2.0968 mL
	40 mM	0.0629 mL	0.3145 mL	0.6290 mL	1.5726 mL
	50 mM	0.0503 mL	0.2516 mL	0.5032 mL	1.2581 mL
	60 mM	0.0419 mL	0.2097 mL	0.4194 mL	1.0484 mL
	80 mM	0.0315 mL	0.1573 mL	0.3145 mL	0.7863 mL
	100 mM	0.0252 mL	0.1258 mL	0.2516 mL	0.6290 mL

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LRRK2 inhibitor 1

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All STAT Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LRRK2 inhibitor 1 Related Classifications

HY-111493 Related Classifications