2. Autophagy
  3. LRRK2 Autophagy Mitophagy
  4. GSK2578215A

GSK2578215A is a potent and highly selective LRRK2 inhibitor, which exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.

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

GSK2578215A Chemical Structure

GSK2578215A Chemical Structure

CAS No. : 1285515-21-0

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10 mM * 1 mL in DMSO
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10 mg USD 88 In-stock
50 mg USD 352 In-stock
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Based on 2 publication(s) in Google Scholar

GSK2578215A Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

GSK2578215A is a potent and highly selective LRRK2 inhibitor, which exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.

In Vitro

GSK2578215A (0-1 μM, 90 min) inhibits Ser910 and Ser935 phosphorylation in HEK293 cells stably transfected with wild-type LRRK2 and LRRK2[G2019S], as well as in mouse Swiss 3T3 cells[1].
GSK2578215A (1 nM, 12 h) induces autophagy (increased level of LC3 and p62 protein) in SH-SY5Y cells[2].
GSK2578215A (1 nM, 12 h) induces Drp1-mediated mitochondrial fission in SH-SY5Y cells, and induces mitophagy (12 and 24 h)[2].
GSK2578215A (1 nM, 24 h) induces oxidative stress, indicated by the accumulation of 4-HNE in SH-SY5Y cells, and induces apoptotical cell death[2].
GSK2578215A (1 μM, 24 h) inhibits homologous recombination in OVCAR8 cells[3].

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

GSK2578215A Related Antibodies
In Vivo

GSK2578215A (5 mg/kg, i.p.) with Olaparib (HY-10162) (50 mg/kg, i.p., T.I.W for 3 weeks) effectively inhibits the tumor growth in mice bearing OVCAR8 xenografts[3].
GSK2578215A (IV, 1 mg/kg, or PO, 10 mg/kg) achieves an exposure in the brain with a brain to plasma ratio of 1.4 (IV) and 2.4 (PO), and shows low oral bioavailability (IV, 12.2%), a half-life of 1.14 h (IV) and plasma exposure (PO, 635.3 h ng/mL, AUClast)[1].

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

Animal Model: mice bearing OVCAR8 xenografts[3]
Dosage: 5 mg/kg, with Olaparib (50 mg/kg)
Administration: i.p., for 3 weeks
Result: Inhibited the tumor growth and increased DNA damage in tumors more potently than Olaparib or GSK2578215A alone.
Molecular Weight

399.42

Formula

C24H18FN3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC1=NC=CC(C2=CC(C(NC3=CC=CN=C3)=O)=C(OCC4=CC=CC=C4)C=C2)=C1
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 (125.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5036 mL 12.5182 mL 25.0363 mL
5 mM 0.5007 mL 2.5036 mL 5.0073 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 2.5036 mL 12.5182 mL 25.0363 mL 62.5908 mL
5 mM 0.5007 mL 2.5036 mL 5.0073 mL 12.5182 mL
10 mM 0.2504 mL 1.2518 mL 2.5036 mL 6.2591 mL
15 mM 0.1669 mL 0.8345 mL 1.6691 mL 4.1727 mL
20 mM 0.1252 mL 0.6259 mL 1.2518 mL 3.1295 mL
25 mM 0.1001 mL 0.5007 mL 1.0015 mL 2.5036 mL
30 mM 0.0835 mL 0.4173 mL 0.8345 mL 2.0864 mL
40 mM 0.0626 mL 0.3130 mL 0.6259 mL 1.5648 mL
50 mM 0.0501 mL 0.2504 mL 0.5007 mL 1.2518 mL
60 mM 0.0417 mL 0.2086 mL 0.4173 mL 1.0432 mL
80 mM 0.0313 mL 0.1565 mL 0.3130 mL 0.7824 mL
100 mM 0.0250 mL 0.1252 mL 0.2504 mL 0.6259 mL
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GSK2578215A 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:

GSK2578215A1285515-21-0LRRK2AutophagyMitophagyLeucine-rich repeat kinase 2Mitochondrial Autophagy3T3 cellOVCAR8 xenografthomologous recombinationSH-SY5YInhibitorinhibitorinhibit

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