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AUTACs

Autophagy-targeting chimeras (AUTACs) contain a guanine tag and a specific binder of an intracellular target of interest. AUTACs both downregulated cytosolic proteins and promoted targeted mitochondrial turnover via mitophagy. Mitochondria-targeted AUTAC (mito-AUTAC) treatment significantly improved mitochondrial activities in Down syndrome (DS)-derived fibroblast cells. This AUTAC technology may hold promise as the first autophagy-inducing agent with cargo specificity.

TSPO ligand-2 
T600151160640-95-8
TSPO ligand-2 (Carbonic acid) is a ligand of AUTAC1 which contains a p-fluorobenzylguanine and a Fumagillol moiety.
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AUTAC1
T740252241669-09-8
AUTAC1 is a MetAP2-targeted autophagy-mediated degrader (AUTAC) with potential anticancer activity that degrades MetAP2 and FKBP12 proteins and can be used to synthesize PROTAC.
  • $506
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Cys-C-cGMP
T826322241669-85-0
Cys-C-cGMP serves as an autophagy tag for AUTACs (autophagy-targeting chimeras). It enhances K63-linked ubiquitination of mitochondria within HeLa cells [1].
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PDL1 degrader-2
T201649
PD-L1degrader-2 (Compound B3) is an orally effective AUTAC degrader that degrades PD-L1 via the autophagy-lysosome pathway with a DC50 of 0.5 μM. It inhibits the interaction between PD-1 and PD-L1, with an IC50 of 22.8 nM. PD-L1degrader-2 upregulates the expression of Atg9b, Lamp1, and Mitf, activating the autophagy-lysosome system. It exhibits antitumor activity in the CT26 mouse model.
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FBnG-(Cys-acetamide)-CH2-PEG3-CH2-CH2-CH2-NH2
T824132241669-84-9
FBnG-(Cys-acetamide)-CH2-PEG3-CH2-CH2-CH2-NH2 serves as a linker for AUTAC4, a compound comprising a p-fluorobenzylguanine (FBnG) unit and a phenylindole moiety, capable of inducing K63-linked polyubiquitination and subsequent degradation of mitochondria within HeLa cells [1].
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TSPO ligand-3
T809282241669-89-4
TSPO ligand-3, functioning as an AUTAC2 ligand, incorporates both a p-fluorobenzylguanine (FBnG) and a synthetic ligand of FKBP (SLF) moiety, leading to the substantial inhibition of FKBP12 in HeLa cells [1].
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