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Bisindolylmaleimide IX, 1 mg  

Bisindolylmaleimide IX, 1 mg

Bisindolylmaleimide IX, Methanesulfonate Salt

Bisindolylmaleimide IX (Ro 31-8220) is a ATP-competitive PKC inhibitor
Synonyms: Ro 31-8220, Ro31-8220, Ro 318220, Ro318220, BIM IX, BIM-9, Bis IX, CAS number: 125314-64-9


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Background: Bisindolylmaleimide IX (Ro 31-8220) is a selective and ATP-competitive PKC inhibitor with an IC50 of 10 nM, whereas the IC50 for the inhibition of PKA is 900 nM. The IC50 values for the inhibition of the group A PKCs range from 5-27 nM and that for PKCε is 24 nM. Ro 31-8220 inhibits growth factor-stimulated expression of MKP-1 and c-Fos but strongly stimulated c-Jun expression, even in the absence of growth factors. Ro 31-8220 strongly stimulates the stress-activated protein kinase JNK1 in a PKC-independent manner.

Chemical formula: C25H23N5O2S . CH4O3S
Molecular weight: 553.7 g/mol
Purity: >90%
Appearance: Orange to red microcrystalline solid
Solubility: Soluble in DMSO, ethanol and water
CAS number: 125314-64-9

Product specific literature references:

Davis PD, Elliott LH, Harris W, Hill CH, Hurst SA, Keech E, Kumar MK, Lawton G, Nixon JS, Wilkinson SE (1992) "Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity" J. Med. Chem. 35(6):994-1001

Wilkinson SE, Parker PJ, Nixon JS (1993) "Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C" Biochem. J. 294 ( Pt 2):335-7

Bit RA, Davis PD, Elliott LH, Harris W, Hill CH, Keech E, Kumar H, Lawton G, Maw A, Nixon JS, et al. (1993) "Inhibitors of protein kinase C 3. Potent and highly selective bisindolylmaleimides by conformational restriction" J. Med. Chem. 36(1):21-9

Dieter P, Fitzke E (1991) "RO 31-8220 and RO 31-7549 show improved selectivity for protein kinase C over staurosporine in macrophages" Biochem. Biophys. Res. Commun. 181 (1): 396-401

Keller HU, Niggli V (1993) "The PKC-inhibitor Ro 31-8220 selectively suppresses PMA- and diacylglycerol-induced fluid pinocytosis and actin polymerization in PMNs" Biochem. Biophys. Res. Commun. 194 (3): 1111-6

Beltman J, McCormick F, Cook SJ (1996) "The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase" J. Biol. Chem. 271(43):27018-24

Budworth J, Davies R, Malkhandi J, Gant TW, Ferry DR, Gescher A (1996) "Comparison of staurosporine and four analogues: their effects on growth, rhodamine 123 retention and binding to P-glycoprotein in multidrug-resistant MCF-7/Adr cells" Br. J. Cancer. 3 (9):1063-8

Harris TE, Persaud SJ, Jones PM (1996) "Atypical isoforms of PKC and insulin secretion from pancreatic beta-cells: evidence using Go 6976 and Ro 31-8220 as PKC inhibitors" Biochem. Biophys. Res. Commun. 227 (3): 672-6

Yeo EJ, Provost JJ, Exton JH (1997) "Dissociation of tyrosine phosphorylation and activation of phosphoinositide phospholipase C induced by the protein kinase C inhibitor Ro-31-8220 in Swiss 3T3 cells treated with platelet-derived growth factor" Biochim. Biophys. Acta 1356 (3): 308-20

Begemann M, Kashimawo SA, Lunn RM, Delohery T, Choi YJ, Kim S, Heitjan DF, Santella RM, Schiff PB, Bruce JN, Weinstein IB (1998) "Growth inhibition induced by Ro 31-8220 and calphostin C in human glioblastoma cell lines is associated with apoptosis and inhibition of CDC2 kinase" Anticancer Res.18(5A):3139-52

Hers I, Tavare JM, Denton RM (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(3):433-6.

Standaert ML, Bandyopadhyay G, Antwi EK, Farese RV (1999) "RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of insulin" Endocrinology 140(5):2145-51

Lingameneni R, Vysotskaya TN, Duch DS, Hemmings HC Jr (2000) "Inhibition of voltage-dependent sodium channels by Ro 31-8220, a \'specific\' protein kinase C inhibitor" FEBS Lett. 473(2):265-8

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.