GSK2578215A
Based on 4 publication(s) in Google Scholar
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.
- Purity: 99.82%
- CAS No.: 1285515-21-0
- Formula: C24H18FN3O2
- Molecular Weight:399.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK2578215A
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Biological Activity
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 (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.
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Animal Model:mice bearing OVCAR8 xenografts[3]
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Dosage:5 mg/kg, with Olaparib (50 mg/kg)
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Administration:i.p., for 3 weeks
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Result:Inhibited the tumor growth and increased DNA damage in tumors more potently than Olaparib or GSK2578215A alone.
Chemical Information
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CAS No. 1285515-21-0
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Appearance Solid
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Molecular Weight 399.42
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Formula C24H18FN3O2
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Color Light yellow to yellow
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SMILES
FC1=NC=CC(C2=CC(C(NC3=CC=CN=C3)=O)=C(OCC4=CC=CC=C4)C=C2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Autophagy
2025 Aug 28:1-15. PMID: 40851277 -
Int Immunopharmacol
Inhibition of LRRK2 alleviates LPS-induced hippocampal pericyte loss and depressive-like behaviors through suppressing the RIPK1-mediated necroptosis pathway. [Abstract]2026 Apr 15:175:116414. PMID: 41740343 -
J Vis Exp
Rab10 Phosphorylation Detection by LRRK2 Activity Using SDS-PAGE with a Phosphate-binding Tag. [Abstract]2017 Dec 14:(130):56688. PMID: 29286425 -
Solvent & Solubility
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)
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.
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.
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.
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- 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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Handling Instructions (2659 KB)
References
[1]. Reith AD, et al. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5625-9. [Content Brief]
[2]. Saez-Atienzar S, et al. The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. Cell Death Dis. 2014 Aug 14;5(8):e1368. [Content Brief]
[3]. Chen L, et al. LRRK2 inhibition potentiates PARP inhibitor cytotoxicity through inhibiting homologous recombination-mediated DNA double strand break repair. Clin Transl Med. 2021 Mar;11(3):e341. [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, 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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