TSPO ligand-1

• CAT Number: I043342
• CAS Number: 4560-08-1
• Molecular Formula: C16H10ClNO2
• Molecular Weight: 283.71
• Purity: ≥95%
• Synonyms: 2-oxo-2-(2-phenyl-1H-indol-3-yl)acetyl chloride
• InChI: InChI=1S/C16H10ClNO2/c17-16(20)15(19)13-11-8-4-5-9-12(11)18-14(13)10-6-2-1-3-7-10/h1-9,18H
• InChIKey: DREHVYWKTXGDBS-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)C2=C(C3=CC=CC=C3N2)C(=O)C(=O)Cl

TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration[1][2].
TSPO ligand-1 gene is induced to increase expression in the context of selective activation of neurons in male C57Bl6/N mice. Moreover, neuronal activation under physiological and psychopharmacological conditions also results in increased TSPO levels in adult mice[2].
TSPO ligand-1 can serve as the sole marker of glial cell activity in Alzheimer’s disease thus tracking the formation of different neural cells[3].
TSPO ligand-1 can regulate mitochondrial fatty acid oxidation (FAO) and thus effects mitochondrial energy homeostasis in MA-10 Leydig cell line[4].

Reference

[1]. Takahashi D, et, al. AUTACs: Cargo-Specific Degraders Using Selective Autophagy. Mol Cell. 2019 Dec 5;76(5):797-810.e10.
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[2]. Tina Notter, et al. Neuronal activity increases translocator protein (TSPO) levels. Mol Psychiatry. 2021 Jun;26(6):2025-2037. doi: 10.1038/s41380-020-0745-1. Epub 2020 May 12.
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[3]. Benjamin B Tournier, et al. Astrocytic TSPO Upregulation Appears Before Microglial TSPO in Alzheimer’s Disease. J Alzheimers Dis. 2020;77(3):1043-1056. doi: 10.3233/JAD-200136.
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[4]. Lan N Tu, et al. Translocator Protein (TSPO) Affects Mitochondrial Fatty Acid Oxidation in Steroidogenic Cells. Endocrinology. 2016 Mar;157(3):1110-21. doi: 10.1210/en.2015-1795. Epub 2016 Jan 7.
 [Content Brief]