908351-31-5
Chemical Structure
Sotrastaurin acetate
Synonym(s): AEB071 acetate
- CAS No.: 908351-31-5
- Formula:C27H26N6O4
- Molecular Weight:498.53
IUPAC Name: 3-(1H-indol-3-yl)-4-(2-(4-methylpiperazin-1-yl)quinazolin-4-yl)-1H-pyrrole-2,5-dione acetate
InChIKey: RVEUYBMXVVDLFO-UHFFFAOYSA-N
SMILES: O=C(C)O.O=C1NC(C(C2=CNC3=C2C=CC=C3)=C1C4=C5C=CC=CC5=NC(N6CCN(CC6)C)=N4)=O
Biological Activity: 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].
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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. | |||||||||||||||||||||
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References
- [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]
