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Chemical Compound Review

AG-K-56845     (3S,6S,9S,12R)-3-butan-2-yl- 6-[(1...

Synonyms: AC1LAG0Z, CTK6C6606, Ambotz183506-66-3
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Disease relevance of apicidin


High impact information on apicidin


Biological context of apicidin

  • We also demonstrate that knockdown of SULF1 with shRNA constructs up-regulates phosphorylation of AKT and Erk and attenuates apicidin-induced apoptosis [6].
  • Taken together, the results suggest that induction of histone hyperacetylation by apicidin is responsible for the antiproliferative activity through selective induction of genes that play important roles in the cell cycle and cell morphology [9].
  • In parallel, apicidin treatment leads to histone hyperacetylation in the IL-8 promoter region independent of NF-kappaB signaling pathway, which is not sufficient for full transcription of IL-8 gene [8].
  • The antiproliferative activity of apicidin on HeLa cells was accompanied by morphological changes, cell cycle arrest at G1 phase, and accumulation of hyperacetylated histone H4 in vivo as well as inhibition of partially purified HDAC in vitro [9].
  • We previously reported that apicidin arrested human cancer cell growth through selective induction of p21(WAF1/Cip1) [10].

Anatomical context of apicidin


Associations of apicidin with other chemical compounds


Gene context of apicidin


Analytical, diagnostic and therapeutic context of apicidin


  1. Induction of apoptosis by apicidin, a histone deacetylase inhibitor, via the activation of mitochondria-dependent caspase cascades in human Bcr-Abl-positive leukemia cells. Cheong, J.W., Chong, S.Y., Kim, J.Y., Eom, J.I., Jeung, H.K., Maeng, H.Y., Lee, S.T., Min, Y.H. Clin. Cancer Res. (2003) [Pubmed]
  2. A hemorrhagic factor (Apicidin) produced by toxic Fusarium isolates from soybean seeds. Park, J.S., Lee, K.R., Kim, J.C., Lim, S.H., Seo, J.A., Lee, Y.W. Appl. Environ. Microbiol. (1999) [Pubmed]
  3. Possible mechanism of action of the histone deacetylase inhibitors for the induction of differentiation of HL-60 clone 15 cells into eosinophils. Ishihara, K., Hong, J., Zee, O., Ohuchi, K. Br. J. Pharmacol. (2004) [Pubmed]
  4. Apicidin is a histone deacetylase inhibitor with anti-invasive and anti-angiogenic potentials. Kim, S.H., Ahn, S., Han, J.W., Lee, H.W., Lee, H.Y., Lee, Y.W., Kim, M.R., Kim, K.W., Kim, W.B., Hong, S. Biochem. Biophys. Res. Commun. (2004) [Pubmed]
  5. Apicidin, a novel histone deacetylase inhibitor, has profound anti-growth activity in human endometrial and ovarian cancer cells. Ueda, T., Takai, N., Nishida, M., Nasu, K., Narahara, H. Int. J. Mol. Med. (2007) [Pubmed]
  6. SULF1 inhibits tumor growth and potentiates the effects of histone deacetylase inhibitors in hepatocellular carcinoma. Lai, J.P., Yu, C., Moser, C.D., Aderca, I., Han, T., Garvey, T.D., Murphy, L.M., Garrity-Park, M.M., Shridhar, V., Adjei, A.A., Roberts, L.R. Gastroenterology (2006) [Pubmed]
  7. Induction of fetal hemoglobin expression by the histone deacetylase inhibitor apicidin. Witt, O., Monkemeyer, S., Rönndahl, G., Erdlenbruch, B., Reinhardt, D., Kanbach, K., Pekrun, A. Blood (2003) [Pubmed]
  8. Activation of NF-kappaB by HDAC inhibitor apicidin through Sp1-dependent de novo protein synthesis: its implication for resistance to apoptosis. Kim, Y.K., Lee, E.K., Kang, J.K., Kim, J.A., You, J.S., Park, J.H., Seo, D.W., Hwang, J.W., Kim, S.N., Lee, H.Y., Lee, H.W., Han, J.W. Cell Death Differ. (2006) [Pubmed]
  9. Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Han, J.W., Ahn, S.H., Park, S.H., Wang, S.Y., Bae, G.U., Seo, D.W., Kwon, H.K., Hong, S., Lee, H.Y., Lee, Y.W., Lee, H.W. Cancer Res. (2000) [Pubmed]
  10. Apicidin, a histone deacetylase inhibitor, induces apoptosis and Fas/Fas ligand expression in human acute promyelocytic leukemia cells. Kwon, S.H., Ahn, S.H., Kim, Y.K., Bae, G.U., Yoon, J.W., Hong, S., Lee, H.Y., Lee, Y.W., Lee, H.W., Han, J.W. J. Biol. Chem. (2002) [Pubmed]
  11. The histone deacetylase inhibitor MS-275 promotes differentiation or apoptosis in human leukemia cells through a process regulated by generation of reactive oxygen species and induction of p21CIP1/WAF1 1. Rosato, R.R., Almenara, J.A., Grant, S. Cancer Res. (2003) [Pubmed]
  12. Apicidin potentiates the imatinib-induced apoptosis of Bcr-Abl-positive human leukaemia cells by enhancing the activation of mitochondria-dependent caspase cascades. Kim, J.S., Jeung, H.K., Cheong, J.W., Maeng, H., Lee, S.T., Hahn, J.S., Ko, Y.W., Min, Y.H. Br. J. Haematol. (2004) [Pubmed]
  13. Histone deacetylase inhibitor FK228 is a potent inducer of human fetal hemoglobin. Cao, H., Stamatoyannopoulos, G. Am. J. Hematol. (2006) [Pubmed]
  14. Additive effect of apicidin and doxorubicin in sulfatase 1 expressing hepatocellular carcinoma in vitro and in vivo. Lai, J.P., Sandhu, D.S., Moser, C.D., Cazanave, S.C., Oseini, A.M., Shire, A.M., Shridhar, V., Sanderson, S.O., Roberts, L.R. J. Hepatol. (2009) [Pubmed]
  15. Involvement of HDAC1 and the PI3K/PKC signaling pathways in NF-kappaB activation by the HDAC inhibitor apicidin. Kim, Y.K., Seo, D.W., Kang, D.W., Lee, H.Y., Han, J.W., Kim, S.N. Biochem. Biophys. Res. Commun. (2006) [Pubmed]
  16. Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells. Hong, J., Ishihara, K., Yamaki, K., Hiraizumi, K., Ohno, T., Ahn, J.W., Zee, O., Ohuchi, K. Cancer Lett. (2003) [Pubmed]
  17. Development of a liquid chromatography/electrospray tandem mass spectrometry assay for the quantification of apicidin, a novel histone deacetylase inhibitor, in rat serum: application to a pharmacokinetic study. Shin, B.S., Kim, J., Yoon, C.H., Kim, C.H., Park, E.H., Han, J.W., Yoo, S.D. Rapid Commun. Mass Spectrom. (2005) [Pubmed]
  18. Transcriptional activation of p21(WAF1/CIP1) by apicidin, a novel histone deacetylase inhibitor. Kim, J.S., Lee, S., Lee, T., Lee, Y.W., Trepel, J.B. Biochem. Biophys. Res. Commun. (2001) [Pubmed]
  19. Pharmacokinetics of a novel histone deacetylase inhibitor, apicidin, in rats. Shin, B.S., Chang, H.S., Park, E.H., Yoon, C.H., Kim, H.Y., Kim, J., Ryu, J.K., Zee, O.P., Lee, K.C., Cao, D., Yoo, S.D. Biopharmaceutics & drug disposition. (2006) [Pubmed]
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