Sotrastaurin acetate
Based on 23 publication(s) in Google Scholar
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.
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- CAS 番号: 908351-31-5
- 分子式: C27H26N6O4
- 分子量:498.53
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Sotrastaurin acetate
More- Signal Transduct Target Ther. 2025 Jul 18;10(1):236. [Abstract]
- Cancer Res. 2015 Nov 1;75(21):4538-47. [Abstract]
- Nat Commun. 2026 Mar 15;17(1):4002. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Death Differ. 2026 Jun 26. [Abstract]
- Mol Ther Oncolytics. 2018 Aug 29:11:1-13. [Abstract]
- NPJ Breast Cancer. 2023 Dec 2;9(1):97. [Abstract]
- Antioxidants (Basel). 2021 Nov 26;10(12):1898. [Abstract]
- Cell Rep. 2024 Dec 3;43(12):115026. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Cancers (Basel). 2023 Mar 6;15(5):1624. [Abstract]
- Mol Cell Biochem. 2021 Jul;476(7):2729-2738. [Abstract]
- Microbiol Spectr. 2022 Oct 26;10(5):e0105622. [Abstract]
- State University of New York at Stony Brook . 2025.
- bioRxiv. 2025 Jan 1:2024.12.31.630780. [Abstract]
- Ruperto Carola University Heidelberg. 2023 Jun 1.
- bioRxiv. 2023 May 28.
- Research Square Preprint. 2023 May 25.
- J Pers Med. 2021 Sep 11;11(9):906. [Abstract]
- Patent. 20200197325A1
- Biomed Pharmacother. 2019 Sep:117:109165. [Abstract]
- Patent. US20180185302A1.
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生物活性
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:30 mg/kg
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Administration:i.g.; daily; 10 days
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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.
化学情報
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CAS 番号 908351-31-5
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分子量 498.53
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分子式 C27H26N6O4
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SMILES
O=C(C)O.O=C1NC(C(C2=CNC3=C2C=CC=C3)=C1C4=C5C=CC=CC5=NC(N6CCN(CC6)C)=N4)=O
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別名
AEB071 acetate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (23)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Phosphoglycerate dehydrogenase stabilizes protein kinase C delta type mRNA to promote hepatocellular carcinoma progression. [Abstract]2025 Jul 18;10(1):236. PMID: 40681503 -
Cancer Res
2015 Nov 1;75(21):4538-47. PMID: 26420215
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.
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Nat Commun
INSIG1/2 succination mediated by the moonlighting function of ADSL promotes lipogenesis and liver tumorigenesis. [Abstract]2026 Mar 15;17(1):4002. PMID: 41833955 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Death Differ
SUMOylation-stabilized G6PD orchestrates metabolic rewiring for oxidative stress survival and chemoresistance in HCC via a PKCδ-phosphorylation trigger. [Abstract]2026 Jun 26. PMID: 42362742 -
Mol Ther Oncolytics
2018 Aug 29:11:1-13. PMID: 30294666
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).
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NPJ Breast Cancer
Clonal heterogeneity in ER+ breast cancer reveals the proteasome and PKC as potential therapeutic targets. [Abstract]2023 Dec 2;9(1):97. PMID: 38042915 -
Antioxidants (Basel)
2021 Nov 26;10(12):1898. PMID: 34942999 -
Cell Rep
2024 Dec 3;43(12):115026. PMID: 39630579 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Cancers (Basel)
PKCθ Regulates Pituitary Adenoma Bone Invasion by Activating Osteoclast in NF-κB/IL-1β-Dependent Manner. [Abstract]2023 Mar 6;15(5):1624. PMID: 36900414 -
Mol Cell Biochem
Tectoridin inhibits the progression of colon cancer through downregulating PKC/p38 MAPK pathway. [Abstract]2021 Jul;476(7):2729-2738. PMID: 33683556 -
Microbiol Spectr
2022 Oct 26;10(5):e0105622. PMID: 36000889 -
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bioRxiv
Nerve Growth Factor Signaling Tunes Axon Maintenance Protein Abundance and Kinetics of Wallerian Degeneration. [Abstract]2025 Jan 1:2024.12.31.630780. PMID: 39803444 -
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J Pers Med
GPR30 Activation by 17β-Estradiol Promotes p62 Phosphorylation and Increases Estrogen Receptor α Protein Expression by Inducing Its Release from a Complex Formed with KEAP1. [Abstract]2021 Sep 11;11(9):906. PMID: 34575683 -
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Biomed Pharmacother
2019 Sep:117:109165. PMID: 31261030 -
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.
純度とドキュメンテーション
参考文献
[1]. de Weerd A, et al. The protein kinase C inhibitor sotrastaurin allows regulatory T cell function. Clin Exp Immunol. 2014;175(2):296-304. [Content Brief]
[2]. He X, et al. Targeting PKC in human T cells using sotrastaurin (AEB071) preserves regulatory T cells and prevents IL-17 production. J Invest Dermatol. 2014;134(4):975-983. [Content Brief]
[3]. Jing F, et al. AEB-071 Ameliorates Muscle Weakness by Altering Helper T Lymphocytes in an Experimental Autoimmune Myasthenia Gravis Rat Model. Med Sci Monit. 2020;26:e924393. Published 2020 Sep 13. [Content Brief]
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Sotrastaurin acetate 関連分類
HY-10540 関連分類
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