Atg4B-IN-2

• CAT Number: I043879
• CAS Number: 2765008-88-4
• Molecular Formula: C21H30O3
• Molecular Weight: 330.46
• Purity: ≥95%
• Synonyms: (E)-4-oxo-4-(4-undecylphenyl)but-2-enoic acid
• InChI: InChI=1S/C21H30O3/c1-2-3-4-5-6-7-8-9-10-11-18-12-14-19(15-13-18)20(22)16-17-21(23)24/h12-17H,2-11H2,1H3,(H,23,24)/b17-16+
• InChIKey: XEPLKXYXNJMMCI-WUKNDPDISA-N
• SMILES: CCCCCCCCCCCC1=CC=C(C=C1)C(=O)C=CC(=O)O

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[1].
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[1].
Atg4B-IN-2 (1 and 5 μM; 2 hours) decreases moderately autophagic vesicles at 1 μM, and almost completely inhibits autophagy at 5 μM[1].
Atg4B-IN-2 (5 μM; 2 hours) inhibits Abi-induced autophagy and significantly augments apoptotic cell death and sensitivity to Abi[1].

Reference

[1]. Kudo Y, Endo S, Fujita M, et al. Discovery and Structure-Based Optimization of Novel Atg4B Inhibitors for the Treatment of Castration-Resistant Prostate Cancer. J Med Chem. 2022;65(6):4878-4892.
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