ALEXIS Biochemicals: Bisindolylmaleimide I

ALX-270-049

Revised 13-Nov-06

Bisindolylmaleimide I
SYNONYMS	GF-109203X Gö 6850
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-049-M001		1 mg	45.00 USD
ALX-270-049-M005		5 mg	150.00 USD

Product Specification

FORMULA:	C₂₅H₂₄N₄O₂
MW:	412.5
CAS NUMBER:	133052-90-1
PURITY:	≥98%
APPEARANCE:	Orange solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	MAY BE CARCINOGENIC. HARMFUL.

Product Description

Cell permeable kinase inhibitor with improved selectivity for protein kinase C (PKC) (K_i=10nM) over several serine/threonine and tyrosine kinases as compared to staurosporine (Prod. No. ALX-380-014). Acts as a competetive inhibitor for the ATP-binding site of PKC. Also inhibits telomerase activity in quercetin (Prod. No. ALX-385-001), H-89 (Prod. No. ALX-270-017), or herbimycin A (Prod. No. ALX-350-029) treated NPC-076 cells. Inhibits protein kinase A at much higher concentrations (K_i=2µM).

Product Specific Literature 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) Abstract; Full Text
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) Abstract
The bisindolylmaleimide GF 109203X, a selective inhibitor of protein kinase C, does not inhibit the potentiating effect of phorbol ester on ethanol-induced phospholipase C-mediated hydrolysis of phosphatidylethanolamine: Z. Kiss, et al.; Biochim. Biophys. Acta 1265, 93 (1995) Abstract
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) Abstract
Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; Biochem. Biophys. Res. Commun. 241, 730 (1997) Abstract
Suprabasin, a Novel Epidermal Differentiation Marker and Potential Cornified Envelope Precursor: G.T. Park, et al.; JBC 277, 45195 (2002) Abstract; Full Text

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