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Chemical Compound Review

BIM-1     3-[1-(3- dimethylaminopropyl)indol-3- yl]-4...

Synonyms: Tocris-0741, CHEMBL7463, BIM I, SureCN78990, BIMI0417, ...
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Disease relevance of RBT205 INHIBITOR

  • In contrast to the transient NF-kappa B activation induced by phorbol ester, the permanent NF-kappa B translocation induced by HIV infection was not dependent on PKC isoenzymes alpha and beta as shown by the use of a specific inhibitor (GF 109203X) [1].
  • This study compared the effects of pharmacological inhibition of PKC with either GF 109203X or chelerythrine on persistent pain following noxious chemical stimulation with its effects on mechanical hyperalgesia, which develops in the hindpaw contralateral to an injury produced by noxious thermal stimulation [2].
  • Considering coupling pathways between NTR stimulation and MAPK activation, we observed a partial inhibition by pertussis toxin (PTX) and a complete blockade by the protein kinase C (PKC) inhibitor GF 109203X [3].
  • It has served as synthetic template for a variety of analogues, the indolocarbazoles, UCN-01 and CGP 41251, and the bisindolylmaleimides, Ro 31-8220 and GF 109203X, were investigated as growth inhibitors of human-derived A549 human lung adenocarcinoma cells [4].
  • Topically applied Gö 6850 inhibited phorbol myristate acetate-induced edema, neutrophil influx and vascular permeability in murine epidermis in a dose- and time-dependent manner at levels comparable to indomethacin [5].

Psychiatry related information on RBT205 INHIBITOR


High impact information on RBT205 INHIBITOR


Chemical compound and disease context of RBT205 INHIBITOR

  • Inhibitors of PKC (GF 109203X, chelerythrine), produced significant reductions of nociceptive responses to 2.5% formalin, as well as a significant reduction in the mechanical hyperalgesia in the hindpaw contralateral to a thermal injury [2].
  • Our results also show that manifestation of Li+ effects in human neuroblastoma cells requires the stimulation of muscarinic receptors and activation of PLCs, PKCs, and/or that other staurosporine/H-7/GF 109203X-sensitive protein kinases are involved in the regulation of Ins(1,4,5)P3 during the plateau phase of ACh-stimulation [12].
  • This effect was partially inhibited by Ro 318220, GF 109203X, U73122, and SB203580, and blocked or nearly completely inhibited by PP1, pertussis toxin, LY294002, PD98059, and AACOCF3 [13].

Biological context of RBT205 INHIBITOR


Anatomical context of RBT205 INHIBITOR


Associations of RBT205 INHIBITOR with other chemical compounds

  • The adding of the PKC inhibitors bisindolylmaleimide-I and LY379196, a specific inhibitor of PKC-beta isoforms, normalized nitrotyrosine and reduced 8-OHdG concentration and cell apoptosis in both stable and intermittent high glucose [22].
  • Inhibition of PKC with either GF 109203X (5 microM) or RO 31-8220 (5 microM) or of protein kinase A with H-89 (50 microM) marginally influenced agonist-dependent phosphorylation of either isoform and failed to modulate homologous desensitization of agonist-induced stimulation of inositol phosphate formation [23].
  • A specific protein kinase C (PKC) inhibitor (GF-109203X) reversed the effect of PMA on tyrosine phosphorylation of Cbl and restored the activation-dependent association of Cbl with PI3-K and CrkL [24].
  • Phosphorylation of ERK in response to CCh was mimicked by the protein kinase C (PKC) activator, phorbol myristate acetate (100 nM), but was not altered by the PKC inhibitor GF 109203X (1 microM) [25].
  • A selective inhibitor of PKC, GF 109203X, markedly inhibited the stimulation of p125FAK tyrosine phosphorylation by PDB but had little effect on the response to bombesin, vasopressin, and endothelin [26].

Gene context of RBT205 INHIBITOR

  • Inhibition of protein kinase C (PKC) by GF 109203X failed to block ERK activation by NECA or UTP, however, another PKC inhibitor, Ro 31-8220, which unlike GF 109203X, can block the zeta-isoform, and prevents UTP- but not NECA-induced ERK activation [27].
  • We were unable to show inhibition of the MEKK response by GF 109203X, a protein kinase C-specific inhibitor [28].
  • The depletion of PKC by prolonged treatment with phorbol 12,13 dibutyrate or the inhibition of PKC by GF 109203X failed to inhibit ET-1-induced activation of JNK [29].
  • Inhibitors of protein kinase C (PKC) (Gö 6976 and GF 109203X) completely inhibited TCR-induced susceptibility to Fas ligation, but only partially inhibited TCR-induced cell surface expression of FasL [30].
  • Notably, the PKC inhibitor GF 109203X reduced ERK1/2 phosphorylation, c-Fos accumulation, c-Jun phosphorylation and KSHV reactivation [31].

Analytical, diagnostic and therapeutic context of RBT205 INHIBITOR

  • Constriction to phenylephrine was significantly decreased by U-73122 (1 muM) and GF-109203X (3 muM) at an intraluminal pressure of 10 mmHg [32].
  • Cross-linking assays revealed that the binding activity of a R1 mRNA 3'-untranslated region binding protein (R1BP), which was previously shown to be involved in the regulation of R1 mRNA stability, was significantly elevated after treatment of the cells with GF 109203X, in a dose-dependent manner [33].
  • The activation of cPLA2 and MAP kinase by 20 microM OAG could be inhibited by pretreatment with 1 microM GF-109203X, a selective inhibitor of protein kinase C. Although only OAG activated cPLA2, both OAG and EAG primed for the release of AA mass as determined by gas chromatography/mass spectrometry [34].


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  2. Noxious thermal and chemical stimulation induce increases in 3H-phorbol 12,13-dibutyrate binding in spinal cord dorsal horn as well as persistent pain and hyperalgesia, which is reduced by inhibition of protein kinase C. Yashpal, K., Pitcher, G.M., Parent, A., Quirion, R., Coderre, T.J. J. Neurosci. (1995) [Pubmed]
  3. Activation of mitogen-activated protein kinase couples neurotensin receptor stimulation to induction of the primary response gene Krox-24. Poinot-Chazel, C., Portier, M., Bouaboula, M., Vita, N., Pecceu, F., Gully, D., Monroe, J.G., Maffrand, J.P., Le Fur, G., Casellas, P. Biochem. J. (1996) [Pubmed]
  4. Differential effects of staurosporine analogues on cell cycle, growth and viability in A549 cells. Courage, C., Snowden, R., Gescher, A. Br. J. Cancer (1996) [Pubmed]
  5. Anti-inflammatory properties of Gö 6850: a selective inhibitor of protein kinase C. Jacobson, P.B., Kuchera, S.L., Metz, A., Schächtele, C., Imre, K., Schrier, D.J. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  6. GF 109203X, a selective inhibitor of protein kinase C, impairs retention performance in an operant task. Stemmelin, J., Mathis, C., Ungerer, A. Neuroreport (1999) [Pubmed]
  7. Modulation of monocyte-endothelial cell interactions by platelet microparticles. Barry, O.P., Praticò, D., Savani, R.C., FitzGerald, G.A. J. Clin. Invest. (1998) [Pubmed]
  8. PDGF induction of alpha 2 integrin gene expression is mediated by protein kinase C-zeta. Xu, J., Zutter, M.M., Santoro, S.A., Clark, R.A. J. Cell Biol. (1996) [Pubmed]
  9. Tyrosine phosphorylation of paxillin and focal adhesion kinase by activation of muscarinic m3 receptors is dependent on integrin engagement by the extracellular matrix. Slack, B.E. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  10. Amyloid precursor protein processing is stimulated by metabotropic glutamate receptors. Lee, R.K., Wurtman, R.J., Cox, A.J., Nitsch, R.M. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  11. Tissue factor-dependent vascular endothelial growth factor production by human fibroblasts in response to activated factor VII. Ollivier, V., Bentolila, S., Chabbat, J., Hakim, J., de Prost, D. Blood (1998) [Pubmed]
  12. Phosphoinositide signalling in human neuroblastoma cells: biphasic effect of Li+ on the level of the inositolphosphate second messengers. Los, G.V., Artemenko, I.P., Hokin, L.E. Adv. Enzyme Regul. (1996) [Pubmed]
  13. Endothelial NADPH oxidase: mechanism of activation by low-density lipoprotein. O'Donnell, R.W., Johnson, D.K., Ziegler, L.M., DiMattina, A.J., Stone, R.I., Holland, J.A. Endothelium (2003) [Pubmed]
  14. Modulation of apoptosis of proliferating and differentiating HL-60 cells by protein kinase inhibitors: suppression of PKC or PKA differently affects cell differentiation and apoptosis. Savickiene, J., Gineitis, A., Stigbrand, T. Cell Death Differ. (1999) [Pubmed]
  15. Differential effects of the protein kinase C activator phorbol 12-myristate 13-acetate on calcium responses and secretion in adherent and suspended RBL-2H3 mucosal mast cells. Wolfe, P.C., Chang, E.Y., Rivera, J., Fewtrell, C. J. Biol. Chem. (1996) [Pubmed]
  16. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. Toullec, D., Pianetti, P., Coste, H., Bellevergue, P., Grand-Perret, T., Ajakane, M., Baudet, V., Boissin, P., Boursier, E., Loriolle, F. J. Biol. Chem. (1991) [Pubmed]
  17. Mechanisms of amelioration of glucose-induced endothelial dysfunction following inhibition of protein kinase C in vivo. Booth, G., Stalker, T.J., Lefer, A.M., Scalia, R. Diabetes (2002) [Pubmed]
  18. Involvement of protein kinase C activation and cell survival/ cell cycle genes in green tea polyphenol (-)-epigallocatechin 3-gallate neuroprotective action. Levites, Y., Amit, T., Youdim, M.B., Mandel, S. J. Biol. Chem. (2002) [Pubmed]
  19. Protein kinase D in small cell lung cancer cells: rapid activation through protein kinase C. Paolucci, L., Rozengurt, E. Cancer Res. (1999) [Pubmed]
  20. Signaling pathways involved in IL-8-dependent activation of adhesion through Mac-1. Takami, M., Terry, V., Petruzzelli, L. J. Immunol. (2002) [Pubmed]
  21. Protein kinase C-dependent tyrosine phosphorylation of p130cas in differentiating neuroblastoma cells. Fagerström, S., Påhlman, S., Nånberg, E. J. Biol. Chem. (1998) [Pubmed]
  22. Intermittent high glucose enhances apoptosis related to oxidative stress in human umbilical vein endothelial cells: the role of protein kinase C and NAD(P)H-oxidase activation. Quagliaro, L., Piconi, L., Assaloni, R., Martinelli, L., Motz, E., Ceriello, A. Diabetes (2003) [Pubmed]
  23. Rapid, agonist-dependent phosphorylation in vivo of human thromboxane receptor isoforms. Minimal involvement of protein kinase C. Habib, A., Vezza, R., Créminon, C., Maclouf, J., FitzGerald, G.A. J. Biol. Chem. (1997) [Pubmed]
  24. Protein kinase C activation inhibits tyrosine phosphorylation of Cbl and its recruitment of Src homology 2 domain-containing proteins. Liu, Y., Liu, Y.C., Meller, N., Giampa, L., Elly, C., Doyle, M., Altman, A. J. Immunol. (1999) [Pubmed]
  25. Carbachol stimulates transactivation of epidermal growth factor receptor and mitogen-activated protein kinase in T84 cells. Implications for carbachol-stimulated chloride secretion. Keely, S.J., Uribe, J.M., Barrett, K.E. J. Biol. Chem. (1998) [Pubmed]
  26. Bombesin stimulation of p125 focal adhesion kinase tyrosine phosphorylation. Role of protein kinase C, Ca2+ mobilization, and the actin cytoskeleton. Sinnett-Smith, J., Zachary, I., Valverde, A.M., Rozengurt, E. J. Biol. Chem. (1993) [Pubmed]
  27. A2B adenosine and P2Y2 receptors stimulate mitogen-activated protein kinase in human embryonic kidney-293 cells. cross-talk between cyclic AMP and protein kinase c pathways. Gao, Z., Chen, T., Weber, M.J., Linden, J. J. Biol. Chem. (1999) [Pubmed]
  28. Activation of MEKK by formyl-methionyl-leucyl-phenylalanine in human neutrophils. Mapping pathways for mitogen-activated protein kinase activation. Avdi, N.J., Winston, B.W., Russel, M., Young, S.K., Johnson, G.L., Worthen, G.S. J. Biol. Chem. (1996) [Pubmed]
  29. Endothelin-1 activates c-Jun NH2-terminal kinase in mesangial cells. Araki, S., Haneda, M., Togawa, M., Kikkawa, R. Kidney Int. (1997) [Pubmed]
  30. Regulation of cell surface expression of Fas (CD95) ligand and susceptibility to Fas (CD95)-mediated apoptosis in activation-induced T cell death involves calcineurin and protein kinase C, respectively. Tóth, R., Szegezdi, E., Molnár, G., Lord, J.M., Fésüs, L., Szondy, Z. Eur. J. Immunol. (1999) [Pubmed]
  31. An essential role of ERK signalling in TPA-induced reactivation of Kaposi's sarcoma-associated herpesvirus. Cohen, A., Brodie, C., Sarid, R. J. Gen. Virol. (2006) [Pubmed]
  32. Characteristics of myogenic tone in the rat ophthalmic artery. Ito, I., Jarajapu, Y.P., Grant, M.B., Knot, H.J. Am. J. Physiol. Heart Circ. Physiol. (2007) [Pubmed]
  33. Posttranscriptional regulation of ribonucleotide reductase R1 gene expression is linked to a protein kinase C pathway in mammalian cells. Chen, F.Y., Amara, F.M., Wright, J.A. Biochem. Cell Biol. (1994) [Pubmed]
  34. Comparison of alkylacylglycerol vs. diacylglycerol as activators of mitogen-activated protein kinase and cytosolic phospholipase A2 in human neutrophil priming. Nixon, A.B., Seeds, M.C., Bass, D.A., Smitherman, P.K., O'Flaherty, J.T., Daniel, L.W., Wykle, R.L. Biochim. Biophys. Acta (1997) [Pubmed]
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