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S130

CAS No. : 1160852-22-1

產(chǎn)品活性：S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC₅₀ of 3.24 µM. S130 suppresses autophagy flux.

研究領(lǐng)域：Metabolic Enzyme/Protease  |  Autophagy  |  Apoptosis

作用靶點(diǎn)：Cathepsin  |  Autophagy  |  Apoptosis

In Vitro: S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity.
S130 (10 μM; 6 hours) suppresses autophagy at the early LC3 priming step or late autolysosome degradation stage.
S130 accumulates autolysosomes with more lipidated LC3.
S130 (0-25 μM; 48 hours) induces cell death through inhibiting the activity of ATG4B at a dose higher than 6.3 µM. And such cytotoxicity might not cause cell death through necroptosis.
Nutrient deprivation enhances S130-induced cytotoxicity.
S130 (0-10μM; 24 hours) suppresses approximately 79% of the cleavage of full-length LC3-GST at the 10 µM, while no substrates were processed in ATG4B KO cells. S130 displays obvious inhibitory effects on ATG4B.

In Vivo: S130 (20 mg/kg; i.p.; daily; 3 weeks) suppresses tumor growth, and shows an efficient in vivo antitumor effect with a sound safety on vital organs.

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