Bisindolylmaleimide I - Order from Adipogen

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Product Datasheet

MSDS

Additional Information

Product Data
Synonyms	GF-109203X; Gö 6850; BIM I
Properties
Formula	C₂₅H₂₄N₄O₂
MW	412.5
CAS	133052-90-1
Purity	≥98% (NMR)
Appearance	Orange solid.
Solubility	Soluble in DMSO.
InChi Key	QMGUOJYZJKLOLH-UHFFFAOYSA-N
Product Type	Chemical
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS	Download
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Product Description

Cell permeable kinase inhibitor with improved selectivity for protein kinase C (PKC) (K_i = 10 nM) [1].
Competetive inhibitor for the ATP-binding site of PKC [1].
Anti-inflammatory [2].
Binds to P-glycoprotein [3].
Telomerase activity inhibitor [4].
Potent glycogen synthase kinase-3 (GSK-3) inhibitor [5].
Necrosis inhibitor [6].
Blocks hERG potassium channels [7-9].
Promotes osteoblastogenesis in human mesenchymal stem cells [10].

Product References

The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C: D. Toullec, et al.; J. Biol. Chem. 266, 15771 (1991) Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3- (dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5- dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model: S. Kuchera, et al.; Agents Actions 39, C169 (1993) Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance: V. Gekeler, et al.; Br. J. Cancer 74, 897 (1996) Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; BBRC 241, 730 (1997) The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity: I. Hers, et al. FEBS Lett. 460, 433 (1999) Bisindolylmaleimide I and V inhibit necrosis induced by oxidative stress in a variety of cells including neurons: R. Asakai, et al.; Neurosci. Res. 44 297 (2002) Direct block of hERG potassium channels by the protein kinase C inhibitor bisindolylmaleimide I (GF109203X): D. Thomas, et al.; Cardiovasc. Res. 64, 467 (2004) The protein kinase C inhibitor, bisindolylmaleimide (I), inhibits voltage-dependent K+ channels in coronary arterial smooth muscle cells: W.S. Park, et al.; Life Sci. 77 512 (2005) Effects of the PKC inhibitors chelerythrine and bisindolylmaleimide I (GF 109203X) on delayed rectifier K(+) currents: G. Harmati, et al.; Naunyn Schmiedebergs Arch. Pharmacol. (Epub ahead of print) (2010) Bisindolylmaleimide I enhances osteogenic differentiation: F. Zhou, et al.; Prot. Cell 3, 311 (2012)

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