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PROTAC

E3 Ligase Ligand-Linker Conjugate

Ligands for Target Protein for PROTAC

Target Protein Ligand-Linker Conjugate

(1)

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.

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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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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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