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Chemical Compound Review

Lopac-M-9656     N-(2- methylaminoethyl)isoquinoline- 5...

Synonyms: CHEMBL148333, SureCN1272378, CHEBI:43561, CCG-100640, KST-1A8801, ...
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High impact information on IQS

  • The increase in the low-Km, cGMP-inhibited cAMP phosphodiesterase activity was inhibited when platelets were incubated with the protein kinase inhibitor H-8 prior to treatment with forskolin, suggesting that the stimulation of cAMP phosphodiesterase activity involved a cAMP-dependent phosphorylation [1].
  • Activation of the PTK was blocked when gametes underwent flagellar adhesion in the presence of the protein kinase inhibitor staurosporine, but not in the presence of the cyclic nucleotide-dependent protein kinase inhibitor, H8, which (unlike staurosporine) does not block the increases in cAMP [2].
  • Although the cAMP-dependent protein kinase inhibitor H8 provided a significant protection against receptor down-regulation, the protein kinase C inhibitor GF109203X had no effect [3].
  • The protein kinase inhibitor H-8 blocks the in vivo phosphorylation of H1 without damaging motility, the acrosome reaction or the ability of sperm to fuse with and activate eggs [4].
  • On the other hand, the cGMP-dependent protein kinase inhibitor H-8 was synergistic with CsA in inhibiting the response of lymphocytes to anti-CD3 plus anti-CD28 but only additive for responses to anti-CD3 [5].

Anatomical context of IQS


Associations of IQS with other chemical compounds


Analytical, diagnostic and therapeutic context of IQS


  1. cAMP-mediated phosphorylation of the low-Km cAMP phosphodiesterase markedly stimulates its catalytic activity. Grant, P.G., Mannarino, A.F., Colman, R.W. Proc. Natl. Acad. Sci. U.S.A. (1988) [Pubmed]
  2. Flagellar adhesion between mating type plus and mating type minus gametes activates a flagellar protein-tyrosine kinase during fertilization in Chlamydomonas. Wang, Q., Snell, W.J. J. Biol. Chem. (2003) [Pubmed]
  3. Synergy between tumor necrosis factor alpha and interleukin 1beta in inducing transcriptional down-regulation of muscarinic M2 receptor gene expression. Involvement of protein kinase A and ceramide pathways. Haddad, E.B., Rousell, J., Lindsay, M.A., Barnes, P.J. J. Biol. Chem. (1996) [Pubmed]
  4. CAMP-dependent protein kinase of sea urchin sperm phosphorylates sperm histone H1 on a single site. Porter, D.C., Moy, G.W., Vacquier, V.D. J. Biol. Chem. (1988) [Pubmed]
  5. The effect of the CD28 activation pathway on the immunosuppressive action of cyclosporine. Hess, A.D., Bright, E.C. Transplantation (1991) [Pubmed]
  6. Potentiation of oncogenic N-ras-induced neurite outgrowth and ornithine decarboxylase activity by phorbol dibutyrate and protein kinase inhibitor H-8. Trotta, R.J., Thomson, T.M., Lacal, J.C., Pellicer, A., Burstein, D.E. J. Cell. Physiol. (1990) [Pubmed]
  7. Involvement of cumulus cells stimulated by FSH in chromatin condensation and the activation of maturation-promoting factor in bovine oocytes. Tatemoto, H., Terada, T. Theriogenology (1998) [Pubmed]
  8. Egg jelly induces the phosphorylation of histone H3 in spermatozoa of the sea urchin Arbacia punctulata. Vacquier, V.D., Porter, D.C., Keller, S.H., Aukerman, M. Dev. Biol. (1989) [Pubmed]
  9. Existence of rolipram-sensitive phosphodiesterase in rat megakaryocyte. Akaike, N., Uneyama, H., Kawa, K., Yamashita, Y. Br. J. Pharmacol. (1993) [Pubmed]
  10. The phosphorylation of a putative sperm microtubule-associated protein 2 (MAP2) is uniquely sensitive to regulation. Carr, D.W., Acott, T.S. Biol. Reprod. (1990) [Pubmed]
  11. Participation of cAMP and cAMP-dependent protein kinase in beta-adrenoceptor-mediated interleukin-1 beta mRNA induction in cultured microglia. Tomozawa, Y., Yabuuchi, K., Inoue, T., Satoh, M. Neurosci. Res. (1995) [Pubmed]
  12. Protein kinase A activity and protein phosphorylation during the mouse sperm acrosomal reaction. Kuji, N., Tanaka, Y., Komatsu, S., Yoshimura, Y. Arch. Androl. (2005) [Pubmed]
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