CUR5g

• CAT Number: I042287
• CAS Number: 1370032-20-4
• Molecular Formula: C22H20N2O2
• Molecular Weight: 344.41
• Purity: ≥95%
• Synonyms: (3E,5E)-3-[(4-hydroxyphenyl)methylidene]-5-(1H-indol-3-ylmethylidene)-1-methylpiperidin-4-one
• InChI: InChI=1S/C22H20N2O2/c1-24-13-17(10-15-6-8-19(25)9-7-15)22(26)18(14-24)11-16-12-23-21-5-3-2-4-20(16)21/h2-12,23,25H,13-14H2,1H3/b17-10+,18-11+
• InChIKey: JMVVTYLZZDOERS-ODPUSEOTSA-N
• SMILES: CN1CC(=CC2=CC=C(C=C2)O)C(=O)C(=CC3=CNC4=CC=CC=C43)C1

CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo[1].
CUR5g (0-40 μM, 0-24 h) selectively induces autophagosome accumulation in cancer cells[1].
CUR5g (0-40 μM, 0-24 h) up-regulates LC3B-II and sequestosome 1 (SQSTM1) levels[1].
CUR5g (0-40 μM, 24 h) inhibits proliferation and migration of A549 cells, but dose not induce apoptosis or necrosis[1].
CUR5g (40 mg/kg, Injected via caudal vein, once every 2 days for up to 15 days) exhibits synergistic anticancer effects with Cisplatin (HY-17394) (1 mg/kg) and inhibits autophagic flux in vivo[1].

Reference

[1]. Chen J, et al. CUR5g, a novel autophagy inhibitor, exhibits potent synergistic anticancer effects with cisplatin against non-small-cell lung cancer. Cell Death Discov. 2022 Oct 31;8(1):435.
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