| Bioactivity | 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]. | |||||||||
| Target | IC50: 3.01 μM (GSK-3) | |||||||||
| Invitro | GSK3-IN-3 (VP07)（25 μM；24 小时）在表达 Parkin 的 U2OS-iMLS 细胞中诱导线粒体自噬，但效力有限[1]。GSK3-IN-3（1.56-25 μM；24 小时）导致 U2OS-iMLS-Parkin 细胞发生线粒体分裂和线粒体形态变化[1]。GSK3-IN-3 (VP0.7)（5 μM，10 μM；）在 SH-SY5Y 细胞的帕金森病体外细胞模型中显示出针对 6-OHDA 的神经保护作用[2]。 Immunofluorescence[1] Cell Line: | |||||||||
| Name | GSK3-IN-3 | |||||||||
| CAS | 331963-27-0 | |||||||||
| Formula | C24H35N3O4 | |||||||||
| Molar Mass | 429.55 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| 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. |