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CA-5f
DC12044  (CAS:1370032-19-1)
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250mg USD 1200 in stock
1g USD 2200 in stock
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Fields of Application :
CA-5f is a novel late-stage autophagy inhibitor with potent anti-tumor effect against non-small cell lung cancer.
CAS Number: 1370032-19-1
Purity:

>98%

Molecular Weight: 388.459
Molecular Formula: C24H24N2O3
Quality Control: HPLCNMR LC/MS(Please contact us to get the QC report)
Synonyms: CA-5f,CA 5f,CA5f,1370032-19-1
Chemical Name: (3E,5E)-3-(3,4-dimethoxybenzylidene)-5-[(1H-indol-3-yl)methylene]-1-methylpiperidin-4-one
Storage: 2 years -20C Powder, 2 weeks4C in DMSO,6 months-80C in DMSO
Note: Products for research use only, not for human use
Description:
CA-5f was identified as a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. We found that CA-5f neither impaired the hydrolytic function nor the quantity of lysosomes. Use of an isobaric tag for relative and absolute quantitation (iTRAQ)-based proteomic screen in combination with bioinformatics analysis suggested that treatment of human umbilical vein endothelial cells (HUVECs) with CA-5f for 1 h suppressed the levels of cytoskeletal proteins and membrane traffic proteins. Subsequent studies showed that CA-5f exhibited strong cytotoxicity against A549 non-small cell lung cancer (NSCLC) cells, but low cytotoxicity to normal human umbilical vein endothelial cells (HUVECs), by increasing mitochondrial-derived reactive oxygen species (ROS) production. Moreover, CA-5f effectively suppressed the growth of A549 lung cancer xenograft as a single agent with an excellent tolerance in vivo. Results from western blot, immunofluorescence, and TdT-mediated dUTP nick end labeling (TUNEL) assays showed that CA-5f inhibited autophagic flux, induced apoptosis, and did not affect the level of CTSB (cathepsin B) and CTSD (cathepsin D) in vivo, which were consistent with the in vitro data. Collectively, these results demonstrated that CA-5f is a novel late-stage autophagy inhibitor with potential clinical application for NSCLC therapy.
References:
N(C)1C/C(=C\C2C3=C(NC=2)C=CC=C3)/C(=O)/C(=C/C2=CC=C(OC)C(OC)=C2)/C1
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