Atg4B-IN-2

Research use only, not for human use.

Atg4B-IN-2. A potent, selective Atg4B inhibitor with anticancer activity, inhibits both Atg4B and PLA2, enabling autophagy that counteracts the anticancer activity of anti-desiccation-resistant prostate cancer drugs.

Atg4B-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.

Atg4B-IN-2 (compound 21f) (1-10 μM; 2 hours) restores the p62 expression in cells treated with AF (amino acid-free) in a dose-dependent manner.Atg4B-IN-2 (1 and 5 μM; 2 hours) decreases moderately autophagic vesicles at 1 μM, and almost completely inhibits autophagy at 5 μM.Atg4B-IN-2 (5 μM; 2 hours) inhibits Abi-induced autophagy and significantly augments apoptotic cell death and sensitivity to Abi.Western Blot AnalysisCell Line:LNCaP cells (incubated in AF medium)Concentration:1, 2, 5, 10 μM Incubation Time:2 hours (then incubated in AFM for 24 or 3 hours) Result:Restored the p62 expression in cells treated with AF in a dose-dependent manner.Cell Autophagy Assay Cell Line:LNCaP cells (incubated in AF medium) Concentration:1 and 5 μM Incubation Time:2 hours (then incubated in AFM for 24 or 3 hours)Result:Decreased moderately autophagic vesicles at 1 μM, and almost completely inhibited autophagy at 5 μM.

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Metabolic Enzyme/Protease

Phospholipase

Phospholipase | Autophagy

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2765008-88-4

330.46

C21H30O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (302.61 mM; Ultrasonic )

C(/C=C/C(O)=O)(=O)C1=CC=C(CCCCCCCCCCC)C=C1

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(-20℃)

With Ice Pack

≥ 2 years