AS2521780
Based on 1 publication(s) in Google Scholar
AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1214726-89-2
- Fòrmula: C30H41N7OS
- Peso molecular:547.76
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Publications Citing Use of MedChemExpress (MCE) AS2521780
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Actividad biológica
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PKCθ 0.48 nM (IC50) |
PKCε 18 nM (IC50) |
PKCα 160 nM (IC50) |
PKCδ 160 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| 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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1214726-89-2
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Peso molecular 547.76
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
Protocolo
Human peripheral T cells are incubated with AS2521780 and anti-human CD28 (0.5 μg/mL). After 48 h incubation, cell proliferation is detected using a CellTiter-Glo Luminescent Cell Viability Assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AS2521780 or vehicle is orally administered twice daily from Day 1 to 24. On Day 25, the left hind paw of each rat is dissected above the ankle joint and fixed in 10% neutral buffered formalin. After decalcification, the paws are embedded in paraffin, sectioned longitudinally and stained with hematoxylin and eosin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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