For research use only. Not for therapeutic Use.
GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC50 value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA[1][2][3].
GSK3-IN-3 (VP07) (25 μM; 24 h) induces mitophagy in Parkin-expressing U2OS-iMLS cells with restricted potency[1].
GSK3-IN-3 (1.56-25 μM; 24 h) results in mitochondria fission with mitochondrial morphology change in U2OS-iMLS-Parkin cells[1].
GSK3-IN-3 (VP0.7) (5 μM, 10 μM; ) shows neuroprotection against 6-OHDA albeit in a Parkinson’s disease in vitro cellular model in SH-SY5Y cells[2].
| Catalog Number | I041706 |
| CAS Number | 331963-27-0 |
| Synonyms | N’-dodecanoyl-1-ethyl-4-hydroxy-2-oxoquinoline-3-carbohydrazide |
| Molecular Formula | C24H35N3O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H35N3O4/c1-3-5-6-7-8-9-10-11-12-17-20(28)25-26-23(30)21-22(29)18-15-13-14-16-19(18)27(4-2)24(21)31/h13-16,29H,3-12,17H2,1-2H3,(H,25,28)(H,26,30) |
| InChIKey | MHKIYMMTEMNCFE-UHFFFAOYSA-N |
| SMILES | CCCCCCCCCCCC(=O)NNC(=O)C1=C(C2=CC=CC=C2N(C1=O)CC)O |
| Reference | [1]. Maestro I, et al. Phenotypic Assay Leads to Discovery of Mitophagy Inducers with Therapeutic Potential for Parkinson’s Disease. ACS Chem Neurosci. 2021 Dec 15;12(24):4512-4523. [2]. Morales-García JA, et al. Glycogen synthase kinase-3 inhibitors as potent therapeutic agents for the treatment of Parkinson disease. ACS Chem Neurosci. 2013 Feb 20;4(2):350-60. [3]. Palomo V, et al. Exploring the binding sites of glycogen synthase kinase 3. Identification and characterization of allosteric modulation cavities. J Med Chem. 2011 Dec 22;54(24):8461-70. |
