2. Epigenetics TGF-beta/Smad NF-κB
  3. PKC NF-κB
  4. Sotrastaurin acetate

Sotrastaurin (AEB071) acetate is a selective, orally active PKC inhibitor. Sotrastaurin acetate inactivates NF-κB by inhibiting PKC α, β, θ, γ subtypes, thereby reducing the transcription levels of immune response-related genes. Sotrastaurin acetate effectively inhibits alloreactive T cell proliferation, conventional T cell activation, as well as the production of pro-inflammatory cytokines and B lymphocytes. Sotrastaurin acetate also maintains the functional and phenotypic stability of regulatory T cells, enhances Foxp3 expression and restores the balance of helper T lymphocytes. Sotrastaurin acetate can prolong the survival time of allografts, and alleviate inflammatory responses and myasthenic symptoms by reducing anti-AChR antibody levels. Sotrastaurin acetate is widely used in studies related to kidney transplantation, psoriasis and myasthenia gravis.

For research use only. We do not sell to patients.

CAS No. : 908351-31-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Sotrastaurin acetate:

Other Forms of Sotrastaurin acetate:

Sotrastaurin acetate Related Antibodies

Top Publications Citing Use of Products

    Sotrastaurin acetate purchased from MedChemExpress. Usage Cited in: Mol Ther Oncolytics. 2018 Aug 29:11:1-13.  [Abstract]

    Levels of murine APOBEC3 are measured by ELISA (left panel) and western blot (right panel) from B16 cells infected with VSV-GFP at an MOI of 0.01 at 0, 48, or 96 hr after treatment with a control IgG, a polyclonal anti-IFN-β antibody, or AEB071 (10 μM).

    Sotrastaurin acetate purchased from MedChemExpress. Usage Cited in: Patent. US20180185302A1.

    Representative PKC inhibitor treated cancer cell line experiment. Each line is treated with AEB071 (10 μM) or vehicle control for 48 hours prior to analysis. The histogram reports APOBEC3B mRNA levels normalized to the vehicle treated control for each line.

    Sotrastaurin acetate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2015 Nov 1;75(21):4538-47.  [Abstract]

    AEB071 downregulates APOBEC3B in multiple cancer cell lines. The histogram reports APOBEC3B mRNA levels normalized to the vehicle treated control for each line. The dotted line represents a 50% decrease of APOBEC3B expression due to AEB071. The corresponding immunoblots show APOBEC3B and TUBULIN levels. Each line is treated with AEB071 (10 μM) or vehicle control for 48 hours prior to mRNA and protein analysis.

    View All PKC Isoform Specific Products:

    View All Isoforms
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

    View All NF-κB Isoform Specific Products:

    View All Isoforms
    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sotrastaurin (AEB071) acetate is a selective, orally active PKC inhibitor. Sotrastaurin acetate inactivates NF-κB by inhibiting PKC α, β, θ, γ subtypes, thereby reducing the transcription levels of immune response-related genes. Sotrastaurin acetate effectively inhibits alloreactive T cell proliferation, conventional T cell activation, as well as the production of pro-inflammatory cytokines and B lymphocytes. Sotrastaurin acetate also maintains the functional and phenotypic stability of regulatory T cells, enhances Foxp3 expression and restores the balance of helper T lymphocytes. Sotrastaurin acetate can prolong the survival time of allografts, and alleviate inflammatory responses and myasthenic symptoms by reducing anti-AChR antibody levels. Sotrastaurin acetate is widely used in studies related to kidney transplantation, psoriasis and myasthenia gravis[1][2][3].

    In Vitro

    Sotrastaurin acetate (100 ng/mL; 30 minutes) does not attenuate IL-2-induced STAT-5 phosphorylation in CD3+CD4+CD25highCD127low regulatory T cells (Tregs) from healthy donors[2].
    Sotrastaurin acetate (10 μM; 3-6 d) potently inhibits the production of IL-17A and IFNg by stimulated healthy human conventional CD4+CD25? T cells after 3 or 6 days[2].
    Sotrastaurin acetate (1 μM; 7 d) maintains the expression of Foxp3 and CD25 in healthy human CD4+CD25high regulatory T cells stimulated for 7 days, without altering the level of RORgt[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Sotrastaurin acetate Related Antibodies
    In Vivo

    Sotrastaurin (AEB-071) acetate (30 mg/kg; p.o.; daily; for 10 consecutive days) reduces the mortality rate of rats with experimental autoimmune myasthenia gravis to 20%, restores body weight, decreases the Lennon score, and rebalances helper T lymphocyte subsets, with beneficial effects superior to those of Azathioprine (HY-B0256)[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Lewis rats (female, 6-8 weeks of age, immunized with R97-116 peptide, Mycobacterium tuberculosis H37RA, Freund's adjuvant, with boosters at 30, 45, 60 days post-injection)[3]
    Dosage: 30 mg/kg
    Administration: i.g.; daily; 10 days
    Result: Reduced Lennon scores to 1.56.
    Reduced serum anti-AChR antibody levels.
    Lowered mortality rate to 20%.
    Decreased proportions of Th1, Th2, and Th17 lymphocytes to levels significantly lower than untreated EAMG rats.
    Maintained Treg cell proportions similar to untreated EAMG rats.
    Showed statistically significant improvements relative to untreated EAMG rats, and outcomes were superior to AZP-treated EAMG rats.
    Molecular Weight

    498.53

    Formula

    C27H26N6O4
    CAS No.
    SMILES

    O=C(C)O.O=C1NC(C(C2=CNC3=C2C=CC=C3)=C1C4=C5C=CC=CC5=NC(N6CCN(CC6)C)=N4)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Sotrastaurin acetate Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Sotrastaurin908351-31-5AEB071AEB 071AEB-071PKCNF-κBProtein kinase CNuclear factor-κBNuclear factor-kappaBB lymphocytePKC βexperimental autoimmune myasthenia gravis rat modelsPBMCT cellPKC αFoxp3PKC θPKC γInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Sotrastaurin acetate
    Cat. No.:
    HY-10540
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.