For research use only. Not for therapeutic Use.
Apicidin（Cat No.:R055023）is a cyclic tetrapeptide that functions as a potent histone deacetylase (HDAC) inhibitor. By inhibiting HDAC, apicidin promotes the acetylation of histones, leading to relaxed chromatin structure and altered gene expression. This mechanism induces cell cycle arrest and apoptosis, particularly in cancer cells, making apicidin a promising candidate for cancer therapy. It has shown potential in treating various cancers, including leukemia and solid tumors. Apicidin also exhibits antiparasitic activity, particularly against Plasmodium falciparum, the causative agent of malaria, further highlighting its therapeutic versatility.
| Catalog Number | R055023 |
| CAS Number | 183506-66-3 |
| Synonyms | Cyclo[(2S)-2-amino-8-oxodecanoyl-1-methoxy-L-tryptophyl-L-isoleucyl-(2R)-2-piperidinecarbonyl]; Cyclo(8-oxo-L-2-aminodecanoyl-1-methoxy-L-tryptophyl-L-isoleucyl-?D-2-piperidinecarbonyl); Apicidin Ia; OSI 2040; |
| Molecular Formula | C₃₄H₄₉N₅O₆ |
| Purity | ≥95% |
| Target | HDAC |
| Solubility | Limited solubility |
| Storage | Store at -20°C |
| Reference | </br>1:The optimization of cell therapy by combinational application with apicidin-treated mesenchymal stem cells after myocardial infarction. Cho DI, Kang WS, Hong MH, Kang HJ, Kim MR, Kim MC, Kim YS, Ahn Y.Oncotarget. 2017 Apr 27. doi: 10.18632/oncotarget.17471. [Epub ahead of print] PMID: 28498815 Free Article</br>2:Apicidin Inhibited Proliferation and Invasion and Induced Apoptosis via Mitochondrial Pathway in Non-small Cell Lung Cancer GLC-82 Cells. Zhang J, Lai Z, Huang W, Ling H, Lin M, Tang S, Liu Y, Tao Y.Anticancer Agents Med Chem. 2017 Apr 19. doi: 10.2174/1871520617666170419120044. [Epub ahead of print] PMID: 28425856 </br>3:Histone deacetylase inhibitor apicidin increases expression of the α-secretase ADAM10 through transcription factor USF1-mediated mechanisms. Hu XT, Zhu BL, Zhao LG, Wang JW, Liu L, Lai YJ, He L, Deng XJ, Chen GJ.FASEB J. 2017 Apr;31(4):1482-1493. doi: 10.1096/fj.201600961RR. Epub 2016 Dec 21. PMID: 28003340 </br>4:In vitro cytotoxicity evaluation of HDAC inhibitor Apicidin in pancreatic carcinoma cells subsequent time and dose dependent treatment. Bauden M, Tassidis H, Ansari D.Toxicol Lett. 2015 Jul 2;236(1):8-15. doi: 10.1016/j.toxlet.2015.03.017. Epub 2015 Apr 24. PMID: 25917448 </br>5:Apicidin inhibits cell growth by downregulating IGF-1R in salivary mucoepidermoid carcinoma cells. Ahn MY, Ahn JW, Kim HS, Lee J, Yoon JH.Oncol Rep. 2015 Apr;33(4):1899-907. doi: 10.3892/or.2015.3776. Epub 2015 Feb 2. PMID: 25647264 </br>6:Apicidin sensitizes pancreatic cancer cells to gemcitabine by epigenetically regulating MUC4 expression. Ansari D, Urey C, Hilmersson KS, Bauden MP, Ek F, Olsson R, Andersson R.Anticancer Res. 2014 Oct;34(10):5269-76. PMID: 25275019 </br>7:Apicidin F: characterization and genetic manipulation of a new secondary metabolite gene cluster in the rice pathogen Fusarium fujikuroi. Niehaus EM, Janevska S, von Bargen KW, Sieber CM, Harrer H, Humpf HU, Tudzynski B.PLoS One. 2014 Jul 24;9(7):e103336. doi: 10.1371/journal.pone.0103336. eCollection 2014. PMID: 25058475 Free PMC Article</br>8:Quantitative determination of absorption and first-pass metabolism of apicidin, a potent histone deacetylase inhibitor. Shin BS, Yoo SD, Kim TH, Bulitta JB, Landersdorfer CB, Shin JC, Choi JH, Weon KY, Joo SH, Shin S.Drug Metab Dispos. 2014 Jun;42(6):974-82. doi: 10.1124/dmd.113.056713. Epub 2014 Mar 18. PMID: 24644298 Free Article</br>9:Activation of snail and EMT-like signaling via the IKKαβ/NF-κB pathway in Apicidin-resistant HA22T hepatocellular carcinoma cells. Tu CC, Cheng LH, Hsu HH, Chen LM, Lin YM, Chen MC, Lee NH, Tsai FJ, Huang CY, Wu WJ.Chin J Physiol. 2013 Dec 31;56(6):326-33. doi: 10.4077/CJP.2013.BAB158. PMID: 24495179 </br>10:Apicidin-resistant HA22T hepatocellular carcinoma cells strongly activated the Wnt/β-catenin signaling pathway and MMP-2 expression via the IGF-IR/PI3K/Akt signaling pathway enhancing cell metastatic effect. Hsieh CH, Cheng LH, Hsu HH, Ho TJ, Tu CC, Lin YM, Chen MC, Tsai FJ, Hsieh YL, Huang CY.Biosci Biotechnol Biochem. 2013;77(12):2397-404. Epub 2013 Dec 7. PMID: 24317053 Free Article |
