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Bisindolylmaleimide I, HCl (CAS 176504-36-2)

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Alternate Names:
3-[1-(Dimethylaminopropyl)indol-3-yl]-4-(indol-3-yl)maleimide hydrochloride
Application:
Bisindolylmaleimide I, HCl is a water soluble inhibitor for all known isoforms of PKC
CAS Number:
176504-36-2
Purity:
≥98%
Molecular Weight:
448.94
Molecular Formula:
C25H24N4O2•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Bisindolylmaleimide I, HCl is a water soluble form of Bisindolylmaleimide I (sc-24003) a staurosporine (sc-3510) inspired molecule, which may act to display equally potent inhibition, but with vastly superior selectivity for all of the known isoforms of PKC (IC50 = 8-20 nM). Inhibition is competitive with respect to ATP, which suggests that Bisindolylmaleimide I occupies the ATP binding domain of the PKC isoforms. This compound has been used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. Shown to inhibit PKC (protein kinase C) within intact platelets and T cells, Fas-mediated apoptosis, and T cell-mediated autoimmune diseases. Bisindolylmaleimide I, HCl is an inhibitor of PKC alpha, PKC beta, PKCdelta, PKC epsilon and PKC gamma.


Bisindolylmaleimide I, HCl (CAS 176504-36-2) References

  1. Hydrogen peroxide induces contraction and raises [Ca2+]i in canine cerebral arterial smooth muscle: participation of cellular signaling pathways.  |  Yang, ZW., et al. 1999. Naunyn Schmiedebergs Arch Pharmacol. 360: 646-53. PMID: 10619181
  2. The effects of protein kinase C and calmodulin kinase II inhibitors on vestibular compensation in the guinea pig.  |  Sansom, AJ., et al. 2000. Brain Res. 882: 45-54. PMID: 11056183
  3. Purinergic and adrenergic agonists synergize in stimulating vasopressin and oxytocin release.  |  Kapoor, JR. and Sladek, CD. 2000. J Neurosci. 20: 8868-75. PMID: 11102496
  4. Ethanol activates NFkappaB DNA binding and p56lck protein tyrosine kinase in human osteoblast-like cells.  |  Yao, Z., et al. 2001. Bone. 28: 167-73. PMID: 11182374
  5. Transmitter release from Rana pipiens vestibular hair cells via mGluRs: a role for intracellular Ca(++) release.  |  Hendricson, AW. and Guth, PS. 2002. Hear Res. 172: 99-109. PMID: 12361872
  6. The role of several kinases in mice tolerant to delta 9-tetrahydrocannabinol.  |  Lee, MC., et al. 2003. J Pharmacol Exp Ther. 305: 593-9. PMID: 12606657
  7. Protein kinase C is involved in neurokinin receptor modulation of N- and L-type Ca2+ channels in DRG neurons of the adult rat.  |  Sculptoreanu, A. and de Groat, WC. 2003. J Neurophysiol. 90: 21-31. PMID: 12660348
  8. Role of nitric oxide and protein kinase C in the tachyphylaxis to vasopressin in rat aortic rings.  |  Hamel, C., et al. 2005. Life Sci. 77: 1069-81. PMID: 15978263
  9. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.  |  Toullec, D., et al. 1991. J Biol Chem. 266: 15771-81. PMID: 1874734
  10. 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.  |  Kiss, Z., et al. 1995. Biochim Biophys Acta. 1265: 93-5. PMID: 7857990
  11. Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976.  |  Martiny-Baron, G., et al. 1993. J Biol Chem. 268: 9194-7. PMID: 8486620
  12. Protein kinase C mediates Ca2(+)-induced cardioadaptation to ischemia-reperfusion injury.  |  Meldrum, DR., et al. 1996. Am J Physiol. 271: R718-26. PMID: 8853396
  13. Ca2+-independent protein kinase C isoforms may modulate parietal cell HCl secretion.  |  Chew, CS., et al. 1997. Am J Physiol. 272: G246-56. PMID: 9124348
  14. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.  |  Zhou, T., et al. 1999. Nat Med. 5: 42-8. PMID: 9883838

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Bisindolylmaleimide I, HCl, 1 mg

sc-24004
1 mg
$145.00