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Sotrastaurin (AEB071)
Cat No.
CEI-1533
Description
Sotrastaurin is a potent and selective small-molecule inhibitor of protein kinase C (PKC) with Ki value of 0.22 nM for PKCθ.
Product Overview
AEB071 is an inhibitor of protein kinase C (PKC). The PKC inhibitor which can block the T-cell activation has the ability of immune suppression. The protein kinase C (PKC) isoforms is very important in cell signaling, proliferation, differentiation, migration, survival, and death. PKC family has many isoforms. Among the PKC isoforms, PKC isoforms have basal effect on the T cells'activation and other immune cell functions. ABE071 is a potent inhibitor of novel and classical PKC isoforms. Through the inhibition of PKC, AEB071 can depress the activation and proliferation of T-cell and decrease the production of cytokine. ABE071 can also suppress the NK cell activity. Ex vivo stimulation of lymphocytes from subjects exposed to single doses of AEB071 resulted in a dose-dependent inhibition of both lymphocyte proliferation and IL2 mRNA expressionAEB071 is an effective treatment strategy for the cure of autoimmune diseases. According to the Psoriasis Area Severity Index (PASI) score, after 2 weeks'treatment with 300 mg bid AEB071, Clinical severity of psoriasis was reduced up to 69% compared with baseline.
CAS No.
425637-18-9
Molecular Weight
438.48
Purity
0.9838
Storage
Store at-20°C
Synonyms
AEB 071; AEB-071
Targets
PKC
IC50
0.22 nM
Molecular Formula
C25H22N6O2
Chemical Name
3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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