AS2521780
Based on 1 publication(s) in Google Scholar
AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
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- CAS No.: 1214726-89-2
- Formule: C30H41N7OS
- Masse moléculaire:547.76
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) AS2521780
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Activité biologique
Description
IC50 & Target
[1]|
PKCθ 0.48 nM (IC50) |
PKCε 18 nM (IC50) |
PKCα 160 nM (IC50) |
PKCδ 160 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
10 nM
Compound: 34
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Inhibition of PKCtheta in human Jurkat cells assessed as reduction in IL2 production after 14 hrs by luciferase reporter gene assay
Inhibition of PKCtheta in human Jurkat cells assessed as reduction in IL2 production after 14 hrs by luciferase reporter gene assay
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[PMID: 30704835] |
In Vitro
AS2521780 exerts potent inhibition of recombinant human PKCθ enzyme activity (IC50=0.48 nM), which is more than 30-fold higher than that of other PKC isoforms. Further, AS2521780 exerts little or no inhibition on other protein kinases. AS2521780 suppresses CD3/CD28-induced Interleukin-2 (IL-2) gene transcription in Jurkat T cells and proliferation of human primary T cells. AS2521780 also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey peripheral blood mononuclear cells with similar potency[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
Chemical Information
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CAS No. 1214726-89-2
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Masse moléculaire 547.76
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Formule C30H41N7OS
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SMILES
N#CC1=CN=C(NCC2=CC=CN=C2SC)N=C1NC[C@]34C[C@]5([H])[C@@H](NC[C@H]6CC[C@H](O)CC6)[C@@](C4)([H])CC(C5)C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Cycle
The protective effects of curcumin in cerebral ischemia and reperfusion injury through PKC-θ signaling. [Abstract]2021 Mar-Mar;20(5-6):550-560. PMID: 33618616
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AS2521780 Related Classifications
HY-12663 Related Classifications
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