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Chemical Compound Review

CHEMBL1256808     1-[2-(4-methoxyphenyl)-2-[3- (4...

Synonyms: SureCN1920184, S7809_SIGMA, SKF-96365, AK-57391, CTK8E8882, ...
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Disease relevance of AIDS035999


High impact information on AIDS035999

  • The CyaA-mediated [Ca(2+)](i) increase in CD11b(+) J774A.1 monocytes was inhibited by extracellular La(3+) ions but not by nifedipine, SK&F 96365, flunarizine, 2-aminoethyl diphenylborinate, or thapsigargin, suggesting that influx of Ca(2+) into cells was not because of receptor signaling or opening of conventional calcium channels by cAMP [5].
  • Bikunin showed no additive effect on SK&F 96365-mediated suppression of TGF-beta1 expression [6].
  • The oscillation was coupled to the electrical activity corresponding to slow waves, and it depended on Ca(2+) influx through a non-selective cation channel, which was SK&F 96365-sensitive and store-operated [7].
  • As an independent verification of specificity, a marked reduction in MMP-2 gelatinase activity by zymogram was shown after treatment of A2058 cells with SK&F 96365, an unrelated inhibitor of receptor-operated calcium influx [8].
  • Consistent with this, we also showed that the BCR-mediated cyclin D2 induction could be abolished by pretreatment of resting B cells with specific inhibitors of capacitative Ca(2+) entry (SK&F 96365) or PKC (Gö6850) [9].

Biological context of AIDS035999

  • This suggests that the cell cycle block induced by SK&F 96365 is not directly related to its action as an inhibitor of receptor-mediated calcium entry [10].
  • Our findings indicate that SK&F 96365, in addition to its ability to inhibit receptor-triggered Ca2+ influx, offers a new method for imposing a reversible mitosis arrest in hematopoietic cell lines [10].
  • However, SK&F 96365 is not as potent (IC50 around 10 microM) or selective (also inhibits voltage-gated Ca2+ entry) as would be desirable, so caution must be exercised when using this compound [11].
  • There were differences in the effectiveness of lectins to activate cation entry and of SK&F 96365, Gd3+, and modulators of protein phosphorylation to block entry [12].
  • SK&F 96365 and removal of extracellular Ca2+ and Na+ partially inhibited exocytosis [12].

Anatomical context of AIDS035999

  • The effect of SK&F 96365 (1-(beta-[3-(4-methoxyphenyl)propoxyl]-4- methoxyphenethyl)-1H-imidazole hydrochloride), a recently synthesized inhibitor of receptor-mediated calcium entry, was investigated on human hematopoietic cell lines [10].
  • We found that treatment of the T-cell leukemia line Jurkat with SK&F 96365 inhibited the Ca2+ influx triggered by antibodies against the CD3/TCR complex, while the inositol trisphosphate-dependent Ca2+ release from intracellular stores remained intact [10].
  • Similar effects of SK&F 96365 were observed in suspensions of neutrophils and in single endothelial cells [11].
  • Our data show the following: (1) ConA and MLI activate monovalent and divalent cation entry in human neutrophils by a SK&F 96365- and Gd3+-sensitive pathway, presumably nonselective cation channels [12].
  • Voltage-gated Ca2+ entry in fura-2-loaded GH3 (pituitary) cells and rabbit ear-artery smooth-muscle cells held under voltage-clamp was also inhibited by SK&F 96365; however, the ATP-gated Ca2(+)-permeable channel of rabbit ear-artery smooth-muscle cells was unaffected by SK&F 96365 [11].

Associations of AIDS035999 with other chemical compounds

  • LOE 908, but not SK&F 96365, inhibited ET-1-induced AA release in wortmannin-treated CHO-ETAR [13].
  • In the absence of added extracellular Ca(2+), 2-APB, Gd(3+) and SK&F 96365 did not alter the kinetics of the increase in [Ca(2+)](cyt) induced by a concentration of adrenaline or vasopressin that induces continuous Ca(2+) oscillations at the physiological extracellular Ca(2+) concentration [14].
  • 1. Multiple effects of the imidazole compound SK&F 96365 have been evaluated on endothelial cells from human umbilical vein using a combined patch clamp and Ca(2+)-microfluorimetric technique (Fura-2) [15].
  • We thus conclude that LTC(4) induces the contraction of the guinea-pig taenia coli mainly through Ca(2+) influx via both the diltiazem-sensitive and SK&F 96365-sensitive Ca(2+) channels, without affecting either the Ca(2+)-sensitivity or the intracellular Ca(2+) release [16].
  • 1. The proposed blocker of receptor-operated calcium channels, SK&F 96365 was shown to inhibit formation of prostaglandin E2 in two osteoblast-like cell lines, MC3T3-E1 and UMR-106 in a dose-dependent manner at an IC50 of 3-4 microM [17].

Gene context of AIDS035999


Analytical, diagnostic and therapeutic context of AIDS035999

  • The inhibition of [3H]-thymidine incorporation by SK&F 96365 occurred in the same concentration range (IC50: approximately 4 microM) as the blockade of capacitative Ca2+ entry in the E3 retinal organ culture [23].
  • Calmodulin discriminates between the two enantiomers of the receptor-operated calcium channel blocker SK&F 96365: a study using 1H-NMR and chiral HPLC [24].


  1. The class III antiarrhythmic drug amiodarone directly activates pertussis toxin-sensitive G proteins. Hagelüken, A., Nürnberg, B., Harhammer, R., Grünbaum, L., Schunack, W., Seifert, R. Mol. Pharmacol. (1995) [Pubmed]
  2. Ca(2+) influx through nonselective cation channels plays an essential role in endothelin-1-induced mitogenesis in C6 glioma cells. Kawanabe, Y., Hashimoto, N., Masaki, T. Neuropharmacology (2001) [Pubmed]
  3. Nuclear envelope-limited chromatin sheets are part of mitotic death. Erenpreisa, J., Ivanov, A., Cragg, M., Selivanova, G., Illidge, T. Histochem. Cell Biol. (2002) [Pubmed]
  4. Inhibition of human brain tumor cell growth by a receptor-operated Ca2+ channel blocker. Lee, Y.S., Sayeed, M.M., Wurster, R.D. Cancer Lett. (1993) [Pubmed]
  5. Third Activity of Bordetella Adenylate Cyclase (AC) Toxin-Hemolysin: MEMBRANE TRANSLOCATION OF AC DOMAIN POLYPEPTIDE PROMOTES CALCIUM INFLUX INTO CD11b+ MONOCYTES INDEPENDENTLY OF THE CATALYTIC AND HEMOLYTIC ACTIVITIES. Fiser, R., Masín, J., Basler, M., Krusek, J., Spuláková, V., Konopásek, I., Sebo, P. J. Biol. Chem. (2007) [Pubmed]
  6. A Kunitz-type protease inhibitor, bikunin, inhibits ovarian cancer cell invasion by blocking the calcium-dependent transforming growth factor-beta 1 signaling cascade. Kobayashi, H., Suzuki, M., Tanaka, Y., Kanayama, N., Terao, T. J. Biol. Chem. (2003) [Pubmed]
  7. Calcium oscillation linked to pacemaking of interstitial cells of Cajal: requirement of calcium influx and localization of TRP4 in caveolae. Torihashi, S., Fujimoto, T., Trost, C., Nakayama, S. J. Biol. Chem. (2002) [Pubmed]
  8. Calcium influx modulates expression of matrix metalloproteinase-2 (72-kDa type IV collagenase, gelatinase A). Kohn, E.C., Jacobs, W., Kim, Y.S., Alessandro, R., Stetler-Stevenson, W.G., Liotta, L.A. J. Biol. Chem. (1994) [Pubmed]
  9. BCR targets cyclin D2 via Btk and the p85alpha subunit of PI3-K to induce cell cycle progression in primary mouse B cells. Glassford, J., Soeiro, I., Skarell, S.M., Banerji, L., Holman, M., Klaus, G.G., Kadowaki, T., Koyasu, S., Lam, E.W. Oncogene (2003) [Pubmed]
  10. Mitosis-arresting effect of the calcium channel inhibitor SK&F 96365 on human leukemia cells. Nordström, T., Nevanlinna, H.A., Andersson, L.C. Exp. Cell Res. (1992) [Pubmed]
  11. SK&F 96365, a novel inhibitor of receptor-mediated calcium entry. Merritt, J.E., Armstrong, W.P., Benham, C.D., Hallam, T.J., Jacob, R., Jaxa-Chamiec, A., Leigh, B.K., McCarthy, S.A., Moores, K.E., Rink, T.J. Biochem. J. (1990) [Pubmed]
  12. Concanavalin A and mistletoe lectin I differentially activate cation entry and exocytosis in human neutrophils: lectins may activate multiple subtypes of cation channels. Wenzel-Seifert, K., Krautwurst, D., Lentzen, H., Seifert, R. J. Leukoc. Biol. (1996) [Pubmed]
  13. Characterization of Ca2+ channels and G proteins involved in arachidonic acid release by endothelin-1/endothelinA receptor. Kawanabe, Y., Nozaki, K., Hashimoto, N., Masaki, T. Mol. Pharmacol. (2003) [Pubmed]
  14. Evidence that Ca2+-release-activated Ca2+ channels in rat hepatocytes are required for the maintenance of hormone-induced Ca2+ oscillations. Gregory, R.B., Barritt, G.J. Biochem. J. (2003) [Pubmed]
  15. Multiple effects of SK&F 96365 on ionic currents and intracellular calcium in human endothelial cells. Schwarz, G., Droogmans, G., Nilius, B. Cell Calcium (1994) [Pubmed]
  16. The mechanism for the contraction induced by leukotriene C4 in guinea-pig taenia coli. Ieiri, S., Nishimura, J., Hirano, K., Suita, S., Kanaide, H. Br. J. Pharmacol. (2001) [Pubmed]
  17. On the inhibition of prostanoid formation by SK&F 96365, a blocker of receptor-operated calcium entry. Leis, H.J., Zach, D., Huber, E., Ziermann, L., Gleispach, H., Windischhofer, W. Br. J. Pharmacol. (1995) [Pubmed]
  18. Pharmacological characterization of endothelin-induced contraction in the guinea-pig oesophageal muscularis mucosae. Uchida, K., Yuzuki, R., Kamikawa, Y. Br. J. Pharmacol. (1998) [Pubmed]
  19. Effects of extracellular Ca2+ influx on endothelin-1-induced intracellular mitogenic cascades in C6 glioma cells. Kawanabe, Y., Hashimoto, N., Masaki, T. Eur. J. Pharmacol. (2002) [Pubmed]
  20. The neuropeptide head activator induces activation and translocation of the growth-factor-regulated Ca(2+)-permeable channel GRC. Boels, K., Glassmeier, G., Herrmann, D., Riedel, I.B., Hampe, W., Kojima, I., Schwarz, J.R., Schaller, H.C. J. Cell. Sci. (2001) [Pubmed]
  21. Mobilization of protein kinase C in macrophages induced by Listeria monocytogenes affects its internalization and escape from the phagosome. Wadsworth, S.J., Goldfine, H. Infect. Immun. (2002) [Pubmed]
  22. Physiological role of Ca2+-permeable nonselective cation channel in endothelin-1-induced contraction of rabbit aorta. Komuro, T., Miwa, S., Zhang, X.F., Minowa, T., Enoki, T., Kobayashi, S., Okamoto, Y., Ninomiya, H., Sawamura, T., Kikuta, K., Iwamuro, Y., Furutani, H., Hasegawa, H., Uemura, Y., Kikuchi, H., Masaki, T. J. Cardiovasc. Pharmacol. (1997) [Pubmed]
  23. Ca2+ mobilization and capacitative Ca2+ entry regulate DNA synthesis in cultured chick retinal neuroepithelial cells. Sugioka, M., Zhou, W.L., Hofmann, H.D., Yamashita, M. Int. J. Dev. Neurosci. (1999) [Pubmed]
  24. Calmodulin discriminates between the two enantiomers of the receptor-operated calcium channel blocker SK&F 96365: a study using 1H-NMR and chiral HPLC. Reid, D.G., MacLachlan, L.K., Robinson, S.P., Camilleri, P., Dyke, C.A., Thorpe, C.J. Chirality. (1990) [Pubmed]
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