Product Details
| Product Name:
GSK2578215A |
CAS No.:
1285515-21-0 |
| Purity:
99.94% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | GSK2578215A |
| Description | GSK2578215A is a potent and selective LRRK2 kinase inhibitor. |
| Kinase Assay | PFV integration assay: For quantitative strand transfer assays, donor DNA substrate is formed by annealing HPLC grade oligonucleotides 5′-GACTCACTATAGGGCACGCGTCAAAATTCCATGACA and 5′-ATTGTCATG GAATTTTGACGCGTGCCCTATAGTGAGTC. Reactions (40 μL) contains 0.75 μM PFV IN, 0.75 μM donor DNA, 4 nM (300 ng) supercoiled pGEM9-Zf(?) target DNA, 125 mM NaCl, 5 mM MgSO4, 4 μM ZnCl2, 10 mM DTT, 0.8% (vol/vol) DMSO, and 25 mM BisTris propane–HCl, pH 7.45. Raltegravir is added at indicated concentrations. Reactions are initiated by addition of 2 μL PFV IN diluted in 150 mM NaCl, 2 mM DTT, and 10 mM Tris-HCl, pH 7.4, and stopped after 1 hour at 37 °C by addition of 25 mM EDTA and 0.5% (wt/vol) SDS. Reaction products, deproteinized by digestion with 20 μg proteinase K for 30 minutes at 37 °C followed by ethanol precipitation, are separated in 1.5% agarose gels and visualized by staining with ethidium bromide. Integration products are quantified by quantitative real-time PCR, using Platinum SYBR Green qPCR SuperMix and three primers: 5′-CTACTTACTCTAGCTTCCCGGCAAC, 5′-TTCGCCAGTTAATAGTTTGCGCAAC, and 5′-GACTCACTATAGGGCACGCGT. PCR reactions (20 μL) contained 0.5 μM of each primer and 1 μL diluted integration reaction product. Following a 5-min denaturation step at 95 °C, 35 cycles are carried out in a CFX96 PCR instrument, using 10 seconds denaturation at 95 °C, 30 seconds annealing at 56 °C and 1 minutes extension at 68 °C. Standard curves are generated using serial dilutions of WT PFV IN reaction in the absence of INSTI. |
| In vitro | Administering 100 mg/kg intraperitoneally (i.p.) of GSK2578215A inhibits the phosphorylation of Ser910 and Ser935 in the spleen and kidneys of mice, but has no effect in the brain. |
| In vivo | In SH-SY5Y cells, GSK2578215A impairs autophagic flux by altering autophagosome-lysosome fusion and induces mitochondrial autophagy through Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. Furthermore, GSK2578215A induces dose-dependent inhibition of Ser910 and Ser935 phosphorylation in HEK293 cells stably transfected with wild-type LRRK2 and LRRK2 [G2019S], and similarly promotes dose-dependent dephosphorylation of Ser910 and Ser935 in endogenous LRRK2 in mouse Swiss 3T3 cells. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 4.5 mg/mL (11.27 mM), Sonication is recommended.
|
| Keywords | GSK2578215A | LRRK2 | Autophagy | Mitophagy | Mitochondrial Autophagy | Inhibitor | GSK-2578215A | inhibit | Leucine-rich repeat kinase 2 |
| Inhibitors Related | Stavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | Cuproptosis Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Parkinson's Disease Compound Library | Autophagy Compound Library | NO PAINS Compound Library | Mitochondria-Targeted Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$1.00/1g |
VIP6Y
|
Career Henan Chemical Co
|
2019-12-23 |
United States