1214726-89-2
1214726-89-2 structure
- Name: AS2521780
- Chemical Name: AS2521780
- CAS Number: 1214726-89-2
- Molecular Formula: C30H41N7OS
- Molecular Weight: 547.76
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2019-03-04 07:28:01
- Modify Date: 2026-07-01 15:51:14
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AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
| Name | AS2521780 |
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| Description | AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM. |
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| Related Catalog | |
| Target |
PKCθ:0.48 nM (IC50) PKCε:18 nM (IC50) PKCα:160 nM (IC50) PKCδ:160 nM (IC50) |
| 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]. |
| In Vivo | AS2521780 significantly reduces paw swelling in a dose-dependent manner in a rat model of adjuvant-induced arthritis[1]. |
| Cell Assay | 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]. |
| Animal Admin | 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]. |
| References |
| Molecular Formula | C30H41N7OS |
|---|---|
| Molecular Weight | 547.76 |