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AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | 2.726 € | 10-14 weeks | |
50 mg | 3.591 € | 10-14 weeks | |
100 mg | 4.940 € | 10-14 weeks |
Description | AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM). |
Targets&IC50 | PKCα:160 nM, PKCδ:160 nM, PKCθ:0.48 nM, PKCε:18 nM |
In vitro | AS2521780 effectively inhibits CD3/CD28-induced Interleukin-2 (IL-2) gene transcription in Jurkat T cells and the proliferation of human primary T cells. Additionally, it impedes concanavalin A-induced cytokine production in rat splenocytes and monkey peripheral blood mononuclear cells with comparable efficacy[1]. The compound demonstrates a potent inhibition of recombinant human PKCθ enzyme activity, with an IC50 value of 0.48 nM, showcasing more than a 30-fold selective inhibition over other PKC isoforms. Moreover, AS2521780 exhibits minimal or no inhibitory effects on other protein kinases. |
In vivo | AS2521780 markedly diminishes paw swelling through a dose-dependent mechanism in a rat model of adjuvant-induced arthritis[1]. |
Molecular Weight | 547.76 |
Formula | C30H41N7OS |
Cas No. | 1214726-89-2 |
Relative Density. | 1.29 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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