Atg4
Autophagy-related 4
Atg4 is the sole cysteine protease among dozens of Atg proteins and functions as an essential factor in the Atg8 conjugation system. While only one Atg4 is present in yeast, there are four Atg4 homologues (Atg4A, Atg4B, Atg4C, and Atg4D) in human and in mouse with different substrate specificities and catalytic efficiencies. Atg4 cleaves Atg8 at the peptide bond on the glycine residue at the C-terminus, thus allowing the conjugation of Atg8 to phosphatidylethanolamine (PE) with the participation of other autophagy molecules. Atg4 can also serve as a deconjugating enzyme, which cleaves the amide bond of the conjugated Atg8 and releases it from the autophagosomal membrane. The latter step is important for reusing Atg8 upon autophagy completion. Moreover, this deconjugation process may also occur on isolation membrane, which would positively or negatively affect membrane formation.
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Atg4 関連製品 (9)
関連製品 (9)
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NSC 185058
0 ImagesNSC 185058 is an inhibitor of ATG4B, a major cysteine protease. Inhibition of ATG4B using NSC 185058 markedly attenuates autophagic activity.
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FMK 9a
0 ImagesFMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
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LV-320
0 Images製品番号: HY-112711CAS 番号: 2449093-46-1LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 μM and a Kd of 16 μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
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Atg4B activator-1
0 Images製品番号: HY-181936CAS 番号: 3126601-01-9Atg4B activator-1 (Compound 16a) is an allosteric, selective, and orally active ATG4B activator with a Kd of 0.2199 μM. Atg4B activator-1 binds to the allosteric pocket of ATG4B and induces conformational changes. Atg4B activator-1 induces Autophagy. Atg4B activator-1 inhibits the proliferation and migration of triple-negative breast cancer cells. Atg4B activator-1 can be used in studies related to triple-negative breast cancer.
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Atg4B-IN-3
0 Images製品番号: HY-184717Atg4B-IN-3 (compound a25) is a ATG4B inhibitor with a Kd value of 18.01 nM against the human target. Atg4B-IN-3 stably regulates the closed conformation of the loop, prevents substrates from accessing the catalytic site Cys74, and thereby inhibits the proteolytic activity of ATG4B. Atg4B-IN-3 blocks autophagic flux, reduces LC3-II levels, promotes p62 accumulation, disrupts autophagy homeostasis and enhances cell death. Atg4B-IN-3 inhibits cell proliferation, migration and clonogenic survival capacity. Atg4B-IN-3 can be used in studies related to esophageal squamous cell carcinoma.
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Atg4B-IN-2
0 ImagesAtg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition.
