| Identification | Back Directory | [Name]
GF109203X | [CAS]
133052-90-1 | [Synonyms]
BIM 1
CS-1080
G 6850]
Estorra
GO 6850
GF 109203X
GO 6850 HCL
GF-109203X HCL
RBT205 INHIBITOR
GF109203X Go-6850
BISINDOYLMALEIMIDE
BISINDOLYLMALEIMIDE
GF109203X USP/EP/BP
BISINDOLYLMALEIMIDE I
Bisindolylmaleinimide
GF109203X HYDROCHLORIDE
BisindolylmaleimideGF 109203X
BISINDOLYLMALEIMIDE I;GO 6850
InSolution? Bisindolylmaleimide I
Bisindolylmaleimide I (GF 109203X)
BISINDOLYLMALEIMIDE I HYDROCHLORIDE
BisindolylMaleiMide I (free base) [GF-109203X
Bisindolylmaleimide I - CAS 133052-90-1 - Calbiochem
3-(N-[DIMETHYLAMINO]PROPYL-3-INDOLYL)-4-(3-INDOLYL)MALEIMIDE
InSolution Bisindolylmaleimide I - CAS 133052-90-1 - Calbiochem
2-(1-(3-DIMETHYLAMINOPROPYL)-INDOL-3-YL)-3-(INDOL-3-YL)MALEIMIDE
2-[1-(3-DIMETHYLAMINOPROPYL)-1H-INDOL-3-YL]-3-(1H-INDOL-3-YL)-MALEIMIDE
2-[1-(3-DIMETHYLAMINOPROPYL)-1H-INDOL-3-YL]-3-(1H-INDOL-3-YL)MALEIMIDE, HCL
3-[1-[3-(DiMethylaMino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrol-2,5-dione
2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide,hydrochloride
3-[1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL]-4-(1H-INDOL-3-YL)-1H-PYRROLE-2 ,5-DIONE
Bisindolylmaleimide
2-(1-(3-Dimethylaminopropyl)-indol-3-yl)-3-(indol-3-yl)maleimide
1H-Pyrrole-2,5-dione, 3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-
3-(N-[Dimethylamino]propyl-3-indolyl)-4-(3-indolyl)maleimide, Bisindolylmaleimide I, 3-[1-[3-(Dimethylamino)propyl]1H-indol-3-yl]-4-(1Hindol-3-yl)1H-pyrrole-2,5dione | [Molecular Formula]
C25H24N4O2 | [MDL Number]
MFCD00236428 | [MOL File]
133052-90-1.mol | [Molecular Weight]
412.48 |
| Chemical Properties | Back Directory | [Melting point ]
280℃ (decomposition) | [Boiling point ]
685.6±55.0 °C(Predicted) | [density ]
1.30±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C
| [solubility ]
DMSO: ~1 mg/mlsoluble
| [form ]
Liquid | [pka]
8.13±0.60(Predicted) | [color ]
Orange | [Water Solubility ]
Insoluble in water. | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 6 months. |
| Hazard Information | Back Directory | [Description]
GF-109203X (133052-90-1) is a potent and selective protein kinase C inhibitor (IC50 = 10 nM; cAMP-dependent protein kinase IC50 = 2 μM and phosphorylase kinase IC50 = 0.7 μM). Inactive against the tyrosine kinases EGFR, PGDFR and Insulin receptor. Potent inhibitor of GSK-3β in cell lysates (IC50 = 360nM) and GSK-3β immunoprecipitates (IC50 = 170nM) derived from rat epididymal adipocytes.2 Cell permeable. | [Uses]
Potent and selective protein kinase C inhibitor which has been used effectively in platelets, Swiss 3T3 fibroblasts and macrophages. Inhibitory profile: PKC, IC50=0.02μM (inhibits α, I, II and γ subtypes with similar potency); PKA, IC50=2.0μM; phosphorylase kinase, IC50=0.7μM; insulin, EGF and PDGF receptor tyrosine kinases are not inhibited at concentrations up to 50μM. | [Biological Activity]
Very potent and selective inhibitor of protein kinase C, selective for the α and β 1 isoforms (IC 50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μ M for α , β 1, δ , ε , and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC 50 values are 0.6, 4.6, and 33 μ M respectively). Potent antagonist at the 5-HT 3 receptor (K i = 29.5 nM). Anti-inflammatory in vivo . Also available as part of the Mixed Kinase Inhibitor Tocriset™ . | [Biochem/physiol Actions]
A potent and selective competitive inhibitor of protein kinase C (PKC) and of glycogen synthase kinase-3 (GSK-3). Inhibits parathyroid hormone-induced Ca2+ resorption from isolated bone tissue, Staurosporine, another protein kinase inhibitor, actually enhanced Ca2+ resorption elicited by a number of agents, but GF109203X counteracted that enhancement. | [storage]
4°C, protect from light | [References]
1) Toullec, et al. (1991), The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C; J. Biol .Chem. 266 15771
2) Hers, et al. (1999) The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity; FEBS Lett. 460 433 |
|
|