| Identification | Back Directory | [Name]
4-Piperidinone, 3-[(4-hydroxyphenyl)methylene]-5-(1H-indol-3-ylmethylene)-1-methyl-, (3E,5E)- | [CAS]
1370032-20-4 | [Synonyms]
CUR5g
4-Piperidinone, 3-[(4-hydroxyphenyl)methylene]-5-(1H-indol-3-ylmethylene)-1-methyl-, (3E,5E)- | [Molecular Formula]
C22H20N2O2 | [MOL File]
1370032-20-4.mol | [Molecular Weight]
344.41 |
| Chemical Properties | Back Directory | [Boiling point ]
627.5±55.0 °C(Predicted) | [density ]
1.322±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
9.38±0.30(Predicted) | [color ]
Yellow to brown |
| Hazard Information | Back Directory | [Uses]
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.html" class="link-product" target="_blank">Cisplatin (HY-17394) against A549 cells both in vitro and in vivo[1]. | [in vivo]
CUR5g (40 mg/kg, Injected via caudal vein, once every 2 days for up to 15 days) exhibits synergistic anticancer effects with Cisplatin.html" class="link-product" target="_blank">Cisplatin (HY-17394) (1 mg/kg) and inhibits autophagic flux in vivo[1]. | Animal Model: | BALB/c nude mice (4-week-old, A549 cells were subcutaneously injected into the right scapula of each nude mouse)[1] | | Dosage: | 40?mg/kg, CUR5g (40 mg/kg) and Cisplatin (1 mg/kg) | | Administration: | Injected via caudal vein, once every 2 days for up to 15 days | | Result: | Retarded the growth of xenografted tumors, whereas the combination treatment with Cisplatin almost completely inhibited tumor growth. Promoted the cisplatin sensitivity of A549 cells by inhibiting autophagic flux. |
| [References]
[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. DOI:10.1038/s41420-022-01217-9 |
|
|