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Chemical Structure| 480-44-4 Chemical Structure| 480-44-4
Chemical Structure| 480-44-4

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Acacetin shows inhibiton of the proliferation and induction apoptosis for cancer cells. It is a flavonoid purified from the bark of acacia farnesiana with anti-peroxidant, antiarthritic, and anti-inflammatory activities,

Synonyms: 5,7-Dihydroxy-4'-methoxyflavone; LY064233; Acacetin. NSC 76061.

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Product Citations

Product Citations

Yun, Sun ; Lee, Yu-Jin ; Choi, Jiyeon ; Kim, Nam Doo ; Han, Dong Cho ; Kwon, Byoung-Mog

Abstract: Signal transducer and activator of transcription 3 (STAT3) plays a critical role in the formation and growth of human cancer. Therefore, STAT3 is a therapeutic target for cancer drug discovery. Acacetin, a flavone present in various plants, inhibits constitutive and inducible STAT3 activation in STAT3-activated DU145 prostate cancer cells. Acacetin inhibits STAT3 activity by directly binding to STAT3, which we confirmed by a pull-down assay with a biotinylated compound and two level-free methods, namely, a drug affinity responsive target stability (DARTS) experiment and a cellular thermal shift assay (CETSA). Acacetin inhibits STAT3 phosphorylation at the tyrosine 705 residue and nuclear translocation in DU145 cells, which leads to the downregulation of STAT3 target genes. Acacetin then induces apoptosis in a time-dependent manner. Interestingly, acacetin induces the production of reactive oxygen species (ROS) that are not involved in the acacetin-induced inhibition of STAT3 activation because the suppressed p-STAT3 level is not rescued by treatment with GSH or NAC, which are general ROS inhibitors. We also found that acacetin inhibits tumor growth in xenografted nude mice. These results suggest that acacetin, as a STAT3 inhibitor, could be a possible drug candidate for targeting STAT3 for the treatment of cancer in humans.

Keywords: STAT3 inhibitor ; acacetin ; antitumor ; label-free methods ; natural product

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Product Details of Acacetin

CAS No. :480-44-4
Formula : C16H12O5
M.W : 284.26
SMILES Code : O=C1C=C(C2=CC=C(OC)C=C2)OC3=C1C(O)=CC(O)=C3
Synonyms :
5,7-Dihydroxy-4'-methoxyflavone; LY064233; Acacetin. NSC 76061.
MDL No. :MFCD00016936
InChI Key :DANYIYRPLHHOCZ-UHFFFAOYSA-N
Pubchem ID :5280442

Safety of Acacetin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Application In Synthesis of Acacetin

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

  • Downstream synthetic route of [ 480-44-4 ]
 

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