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GF 109203X

  Cat. No.:  DC7132   Featured
Chemical Structure
133052-90-1
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More than 5000 active chemicals with high quality for research!
Field of application
GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 133052-90-1
Chemical Name: Bisindolylmaleimide i
Synonyms: 1H-Pyrrole-2,5-dione,3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-;GF109203X;2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl)maleimide;3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione;Bisindolylmaleimide I;Bisindolylmaleimide I (BIM I,Gö 6850, GF 109203X);Bisindolylmaleimide I (GF 109203X);3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrolyl-2,5-dione;3-{1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL}-4-(1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE;GF-109203X;Go6850;RBT205 INHIBITOR;3-(N-[Dimethylamino]propyl-3-indolyl)-4-(3-indolyl)maleimide;3-[1-[3-(Dimethylamino)propyl]1H-indol-3-yl]-4-(1Hindol-3-yl)1H-pyrrole-2,5dione;3-[1-[3-(Dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrol-2,5-dione;BIM 1;G 6850];GO 6850 HCL;GF-109203X HCL;BISINDOYLMALEIMIDE;BISINDOLYLMALEIMIDE;Bisindolylmaleinimide;GO 6850;GF 109203X;Gö 6850;3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione;L79H6N0V6C;QMGUOJYZJKLOLH-UHFFFAOYSA-N;2-[1-(3-dimethylaminopropyl)indol-3-
SMILES: O=C1C(=C(C(N1[H])=O)C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)C1=C([H])N(C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])C2=C([H])C([H])=C([H])C([H])=C12
Formula: C25H24N4O2
M.Wt: 412.4837
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
In Vivo: Pial arteriole diameter changes are monitored using a closed cranial window in vivo microscopy technique. The pial arteriole dilatory response associated with SNS is decreased by 45%, when comparing DM vs either ND or TR rats. Also, pial arteriolar dilations to topical KCl and NS1619 are largely attenuated in DM rats, but not in ND or TR animals. These responses are completely restored by the acute application of Bisindolylmaleimide I to the brain surface. The PKC inhibitor has no effect on vascular responses in normoglycemic and TR animals. In conclusion, DM-associated chronic impairment of neurovascular coupling may be readily reversed by a PKC-α/β/γ inhibitor or prevented via pancreatic islet transplantation. Specific PCK isoforms (α/β/γ) are believed to be mechanistically linked to the neurovascular uncoupling seen with hyperglycemia[2].
In Vitro: Bisindolylmaleimide I is a competitive inhibitor with respect to ATP (Ki=14 nM) and displays high selectivity for PKC as compared to five different protein kinases. GF 109203X efficiently prevents PKC-mediated phosphorylations of an Mr=47,000 protein in platelets and of an Mr=80,000 protein in Swiss 3T3 cells. GF 109203X inhibits collagen- and a-thrombin-induced platelet aggregation as well as collagen-triggered ATP secretion. However, ADP-dependent reversible aggregation is not modified. In Swiss 3T3 fibroblasts, GF 109203X reverses the inhibition of epidermal growth factor binding induced by phorbol 12,13-dibutyrate and prevents [3H] thymidine incorporation into DNA, only when this is elicited by growth promoting agents which activate PKC[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC9698 Staurosporine Staurosporine is a prototypical potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively.
DC7270 Ro 31-8220 mesylate Ro 31-8220 mesylate (Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.
DC10645 Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
DC8523 LY333531 Hydrochloride(Ruboxistaurin HCl) LY-333,531 Hydrochloride is a potent, selective inhibitor of Protein Kinase C isozymes, PKC beta I (IC50 = 4.7 nM) and PKC beta II (IC50 = 5.9 nM). It is potentially beneficial for cancer research.
DC7835 H-89 2HCl H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II.
DC7660 Go 6983 Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.
DC7132 GF 109203X GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.
DC5057 Enzastaurin (LY317615) Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.
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