A PKC inhibitor
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Bisindolylmaleimide XI (hydrochloride)

Item No. 11073

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione, monohydrochloride
CAS Number
145333-02-4
Synonyms
  • BIM XI
  • Ro 31-0432
Molecular Formula
C28H28N4O2 • HCl
Formula Weight
489.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
SMILES
O=C(NC1=O)C(C2=CNC3=C2C=CC=C3)=C1C4=C5N(CCC(CN(C)C)C5)C6=CC=CC=C64.Cl
InChi Code
InChI=1S/C28H28N4O2.ClH/c1-30(2)15-17-12-13-32-22-11-7-5-9-19(22)24(23(32)14-17)26-25(27(33)29-28(26)34)20-16-31(3)21-10-6-4-8-18(20)21;/h4-11,16-17H,12-15H2,1-3H3,(H,29,33,34);1H
InChi Key
HSPRASOZRZDELU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Bisindolylmaleimide XI (BIM XI) is a selective, cell-permeable protein kinase C (PKC) inhibitor that displays 10-fold greater selectivity for PKCα (IC50 = 9 nM) and 4-fold greater selectivity for PKCβI (IC50 = 28 nM) over Ca2+-independent PKCε (IC50 = 108 nM).1 Inhibition of PKCα by BIM XI and other similar PKC inhibitors has been associated with enhanced cardiac contractility and protection from heart failure.2 BIM XI prevents T-cell activation and proliferation (with IC50s ranging from 30-150 nM) associated with chronic inflammatory responses in vivo.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wilkinson, S.E., Parker, P.J., and Nixon, J.S. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem. J. 294(Pt 2), 335-337 (1993).

    2. Liu, Q., Chen, X., MacDonnell, S.M., et al. PKCα, but not PKCβ or PKCγ, regulates contractility and heart failure susceptibility: Implications for ruboxistaurin as a novel therapeutic approach. Circ. Res. 105(2), 194-200 (2009).

    3. Birchall, A.M., Bishop, J., Bradshaw, D., et al. Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. J. Pharmacol. Exp. Ther. 268(2), 922-929 (1994).