A PKCβ Inhibitor
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PKCβ Inhibitor

Item No. 35494

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[1-[3-(1H-imidazol-1-yl)propyl]-1H-indol-3-yl]-4-(phenylamino)-1H-pyrrole-2,5-dione
CAS Number
257879-35-9
Synonyms
  • Protein Kinase Cβ Inhibitor
Molecular Formula
C24H21N5O2
Formula Weight
411.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 0.25 mg/ml
λmax
226 nm
SMILES
O=C1NC(C(C2=CN(CCCN3C=NC=C3)C4=C2C=CC=C4)=C1NC5=CC=CC=C5)=O
InChi Code
InChI=1S/C24H21N5O2/c30-23-21(22(24(31)27-23)26-17-7-2-1-3-8-17)19-15-29(20-10-5-4-9-18(19)20)13-6-12-28-14-11-25-16-28/h1-5,7-11,14-16H,6,12-13H2,(H2,26,27,30,31)
InChi Key
KIWODJBCHRADND-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    PKCβ inhibitor is an inhibitor of PKCβ1 and PKCβ2 (IC50s = 21 and 5 nM, respectively).1 It is selective for PKCβ1 and PKCβ2 over PKCα, PKCε, and PKCγ (IC50s = 331, 2,807, and >1,000 nM, respectively), as well as JAK1, JAK2, and tyrosine kinase 2 (TYK2; IC50s = 770, 3,850, and 2,310 nM, respectively), but also inhibits JAK3 (IC50 = 17 nM).1,2 PKCβ inhibitor (14 µM) induces apoptosis and inhibits cell cycle progression in 2F7 AIDS-related Burkitt’s lymphoma cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tanaka, M., Sagawa, S., Hoshi, J.-I., et al. Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg. Med. Chem. Lett. 14(20), 5171-5174 (2004).

    2. McDonnell, M.E., Bian, H., Wrobel, J., et al. Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors. Bioorg. Med. Chem. Lett. 24(4), 1116-1121 (2014).

    3. Saba, N.S., and Levy, L.S. Protein kinase C-beta inhibition induces apoptosis and inhibits cell cycle progression in acquired immunodeficiency syndrome-related non-hodgkin lymphoma cells. J. Investig. Med. 60(1), 29-38 (2012).