GSK2578215A
GSK2578215A
CAS: 1285515-21-0
Molecular Formula: C24H18FN3O2
GSK2578215A - Names and Identifiers
GSK2578215A - Physico-chemical Properties
| Molecular Formula | C24H18FN3O2 |
| Molar Mass | 399.42 |
| Density | 1.292±0.06 g/cm3(Predicted) |
| Boling Point | 556.1±50.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| Appearance | powder |
| Color | white to beige |
| pKa | 12.31±0.70(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | GSK2578215A induces a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells, and induces similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells. In SH-SY5Y cells, GSK2578215A impairs the autophagy flux by altering autophagosome–lysosome fusion, and induces mitophagy though induction of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. |
| In vivo study | In vivo, GSK2578215A (100 mg/kg i.p.) inhibits Ser910 and Ser935 phosphorylation in mouse spleen and kidney, but not in brain. |
GSK2578215A - Risk and Safety
| WGK Germany | 3 |
GSK2578215A - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.504 ml | 12.518 ml | 25.036 ml |
| 5 mM | 0.501 ml | 2.504 ml | 5.007 ml |
| 10 mM | 0.25 ml | 1.252 ml | 2.504 ml |
| 5 mM | 0.05 ml | 0.25 ml | 0.501 ml |
Last Update：2024-01-02 23:10:35
GSK2578215A - Reference Information
| biological activity | GSK2578215A is an effective selective LRRK2 kinase inhibitor, and its IC50 for LRRK2 (G2019S) and LRRK2 (WT) is 8.9 nM and 10.9 nM respectively. |
| in vitro study | GSK2578215A induces a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stable transfected into HEK293 cells, and induces similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells. In SH-SY5Y cells, GSK2578215A impairs the autophagy flux by altering autophagosome-lysosome fusion, and induces mitophagy though induction of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. |
| in vivo research | in vivo, GSK2578215A (100 mg/kg I. p.) inhibits Ser910 and Ser935 phosphorylation in mouse spleen and kidney, but not in brain. |
Last Update：2024-04-09 20:49:11
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