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AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $3,020 | 3-6 months | 3-6 months | |
| 50 mg | $3,980 | 3-6 months | 3-6 months | |
| 100 mg | $5,500 | 3-6 months | 3-6 months |
| 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 |
| Smiles | C(NC=1C(C#N)=CN=C(NCC2=C(SC)N=CC=C2)N1)C34C[C@@]5([C@@H](NC[C@@H]6CC[C@@H](O)CC6)[C@](C3)(CC(C4)C5)[H])[H] |
| 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/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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