A PKC and GSK3 inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Sotrastaurin

Item No. 16726

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(1H-indol-3-yl)-4-[2-(4-methyl-1-piperazinyl)-4-quinazolinyl]-1H-pyrrole-2,5-dione
CAS Number
425637-18-9
Synonyms
  • AEB071
Molecular Formula
C25H22N6O2
Formula Weight
438.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
246, 438 nm
SMILES
CN(CC1)CCN1C2=NC3=CC=CC=C3C(C(C(N4)=O)=C(C5=CNC6=C5C=CC=C6)C4=O)=N2
InChi Code
InChI=1S/C25H22N6O2/c1-30-10-12-31(13-11-30)25-27-19-9-5-3-7-16(19)22(28-25)21-20(23(32)29-24(21)33)17-14-26-18-8-4-2-6-15(17)18/h2-9,14,26H,10-13H2,1H3,(H,29,32,33)
InChi Key
OAVGBZOFDPFGPJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $54

    Add

    5 mg

    $223

    Add

    10 mg

    $392

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    Sotrastaurin is a protein kinase C (PKC) inhibitor that displays immunosuppressive activity, blocking T cell activation through the disruption of downstream NF-κB signaling.1,2 In cell-free assays, sotrastaurin was reported to inhibit PKCα, βI, δ, ε, η, and θ with Ki values of 0.95, 0.64, 2.1, 3.2, 1.8, and 0.22 nM, respectively.1 Sotrastaurin can prevent the production of various cytokines by activated T cells, macrophages, and keratinocytes in vitro and has been shown to inhibit an acute allergic contact dermatitis response in rats when dosed orally at 30 mg.3 However, clinical investigation of sotrastaurin for its potential to prevent renal transplant rejection was halted during phase II testing due to high incidence of rejection.4 Sotrastaurin is also reported to activate Wnt/β-catenin signaling via the inhibition of glycogen synthase kinase 3 (IC50s = 229 and 172 nM for α and β isoforms, respectively), which is essential for embryogenesis and adult stem cell maintenance.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Evenou, J.P., Wagner, J., Zenke, G., et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J. Pharmacol. Exp. Ther. 330(3), 792-801 (2009).

    2. Vafadari, R., Kraaijeveld, R., Weimar, W., et al. Tacrolimus inhibits NF-κB activation in peripheral human T cells. PLoS One 8(4), e60784 (2014).

    3. Skvara, H., Dawid, M., Kleyn, E., et al. The PKC inhibitor AEB071 may be a therapeutic option for psoriasis. J. Clin. Invest. 118(9), 3151-3159 (2008).

    4. Hardinger, K.L., and Brennan, D.C. Novel immunosuppressive agents in kidney transplantation. World J. Transplant. 3(4), 68-77 (2013).

    5. Verkaar, F., Blankesteijn, W.M., Smits, J.F.M., et al. β-Galactosidase enzyme fragment complementation for the measurement of Wnt/β-catenin signaling. The FASEB Journal 24(4), 1205-1217 (2010).

    6. Verkaar, F., van der Stelt, M., Blankesteijn, W.M., et al. Discovery of novel small molecule activators of β-catenin signaling. PLoS One 6(4), e19185 (2011).