GSK2578215APotent, selective LRRK2 inhibitor; brain penetrant CAS# 1285515-21-0 |
- GSK256066 2,2,2-trifluoroacetic acid
Catalog No.:BCC1605
CAS No.:1415560-64-3
- Nortadalafil
Catalog No.:BCC1806
CAS No.:171596-36-4
- Bay 60-7550
Catalog No.:BCC1405
CAS No.:439083-90-6
- Oglemilast
Catalog No.:BCC1817
CAS No.:778576-62-8
- AN-2728
Catalog No.:BCC1361
CAS No.:906673-24-3
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1285515-21-0 | SDF | Download SDF |
PubChem ID | 68107965 | Appearance | Powder |
Formula | C24H18FN3O2 | M.Wt | 399.42 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : 50 mg/mL (125.18 mM; Need ultrasonic) | ||
Chemical Name | 5-(2-fluoropyridin-4-yl)-2-phenylmethoxy-N-pyridin-3-ylbenzamide | ||
SMILES | C1=CC=C(C=C1)COC2=C(C=C(C=C2)C3=CC(=NC=C3)F)C(=O)NC4=CN=CC=C4 | ||
Standard InChIKey | WCIGMFCFPXZRMQ-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C24H18FN3O2/c25-23-14-19(10-12-27-23)18-8-9-22(30-16-17-5-2-1-3-6-17)21(13-18)24(29)28-20-7-4-11-26-15-20/h1-15H,16H2,(H,28,29) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Potent LRRK2 inhibitor (IC50 values are 8.9 and 10.1 nM for LRRK2[G2019S] mutant and wild-type LRRK2 respectively). Displays selectivity for LRRK2 over a panel of 460 other kinases. Blocks Ser910 and Ser935 phosphorylation in vitro and in peripheral tissues in vivo. Brain penetrant. |
GSK2578215A Dilution Calculator
GSK2578215A Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.5036 mL | 12.5182 mL | 25.0363 mL | 50.0726 mL | 62.5908 mL |
5 mM | 0.5007 mL | 2.5036 mL | 5.0073 mL | 10.0145 mL | 12.5182 mL |
10 mM | 0.2504 mL | 1.2518 mL | 2.5036 mL | 5.0073 mL | 6.2591 mL |
50 mM | 0.0501 mL | 0.2504 mL | 0.5007 mL | 1.0015 mL | 1.2518 mL |
100 mM | 0.025 mL | 0.1252 mL | 0.2504 mL | 0.5007 mL | 0.6259 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. IC50 value: ~10 nM(wt-LRRK2; LRRK2 G2019S) [1] Target: LRRK2 inhibitor GSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3–1.0 μM in cells and in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg [1].
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.
- Romidepsin (FK228, depsipeptide)
Catalog No.:BCC3597
CAS No.:128517-07-7
- Ophiogenin-3-O-alpha-L-rhaMnopyranosyl-(1→2)-beta-D-glucopyranoside
Catalog No.:BCN1587
CAS No.:128502-94-3
- Methylophioponanone B
Catalog No.:BCN6525
CAS No.:128446-36-6
- 2-Hydroxypropyl-β-cyclodextrin
Catalog No.:BCC6757
CAS No.:128446-35-5
- Gelidoside
Catalog No.:BCN7320
CAS No.:128420-44-0
- Euojaponine D
Catalog No.:BCC8980
CAS No.:128397-42-2
- Hydroprotopine
Catalog No.:BCN6155
CAS No.:128397-41-1
- Hyptadienic acid
Catalog No.:BCN6154
CAS No.:128397-09-1
- MCH (human, mouse, rat)
Catalog No.:BCC6068
CAS No.:128315-56-0
- Cinalukast
Catalog No.:BCC7244
CAS No.:128312-51-6
- MK-8033 hydrochloride
Catalog No.:BCC4040
CAS No.:1283000-43-0
- 2alpha-Hydroxy-8beta-(2-methylbutyryloxy)costunolide
Catalog No.:BCN7319
CAS No.:128286-87-3
- ML167
Catalog No.:BCC5348
CAS No.:1285702-20-6
- Pingpeimine C
Catalog No.:BCN8411
CAS No.:128585-96-6
- Ospemifene
Catalog No.:BCC5557
CAS No.:128607-22-7
- Z(2-Br)-Osu
Catalog No.:BCC2806
CAS No.:128611-93-8
- PyBOP
Catalog No.:BCC2820
CAS No.:128625-52-5
- 1,6-O,O-Diacetylbritannilactone
Catalog No.:BCN7792
CAS No.:1286694-67-4
- FRAX597
Catalog No.:BCC4172
CAS No.:1286739-19-2
- Eucamalduside A
Catalog No.:BCN7321
CAS No.:1287220-29-4
- Kalopanaxsaponin H
Catalog No.:BCN2572
CAS No.:128730-82-5
- Mycophenolate Mofetil
Catalog No.:BCC2290
CAS No.:128794-94-5
- Fmoc-D-Asp(OtBu)-OH
Catalog No.:BCC3471
CAS No.:12883-39-3
- Fargesol
Catalog No.:BCN6421
CAS No.:128855-64-1
The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.[Pubmed:25118928]
Cell Death Dis. 2014 Aug 14;5:e1368.
Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene have been associated with Parkinson's disease, and its inhibition opens potential new therapeutic options. Among the drug inhibitors of both wild-type and mutant LRRK2 forms is the 2-arylmethyloxy-5-subtitutent-N-arylbenzamide GSK257815A. Using the well-established dopaminergic cell culture model SH-SY5Y, we have investigated the effects of GSK2578215A on crucial neurodegenerative features such as mitochondrial dynamics and autophagy. GSK2578215A induces mitochondrial fragmentation of an early step preceding autophagy. This increase in autophagosome results from inhibition of fusion rather than increases in synthesis. The observed effects were shared with LRRK2-IN-1, a well-described, structurally distinct kinase inhibitor compound or when knocking down LRRK2 expression using siRNA. Studies using the drug mitochondrial division inhibitor 1 indicated that translocation of the dynamin-related protein-1 has a relevant role in this process. In addition, autophagic inhibitors revealed the participation of autophagy as a cytoprotective response by removing damaged mitochondria. GSK2578215A induced oxidative stress as evidenced by the accumulation of 4-hydroxy-2-nonenal in SH-SY5Y cells. The mitochondrial-targeted reactive oxygen species scavenger MitoQ positioned these species as second messengers between mitochondrial morphologic alterations and autophagy. Altogether, our results demonstrated the relevance of LRRK2 in mitochondrial-activated pathways mediating in autophagy and cell fate, crucial features in neurodegenerative diseases.
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.[Pubmed:22863203]
Bioorg Med Chem Lett. 2012 Sep 1;22(17):5625-9.
Leucine-rich repeat kinase 2 (LRRK2) is a promising therapeutic target for some forms of Parkinson's disease. Here we report the discovery and characterization of 2-arylmethyloxy-5-subtitutent-N-arylbenzamides with potent LRRK2 activities exemplified by GSK2578215A which exhibits biochemical IC(50)s of around 10 nM against both wild-type LRRK2 and the G2019S mutant. GSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3-1.0 muM in cells and in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100mg/kg.