AS2521780 |
رقم الكتالوجGC31959 |
AS2521780 هو مثبط انتقائي جديد لـ PKCθ مع IC50 من 0.48 نانومتر
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Cas No.: 1214726-89-2
Sample solution is provided at 25 µL, 10mM.
AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
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].
AS2521780 significantly reduces paw swelling in a dose-dependent manner in a rat model of adjuvant-induced arthritis[1].
[1]. Fukahori H, et al. Effect of AS2521780, a novel PKCθ selective inhibitor, on T cell-mediated immunity. Eur J Pharmacol. 2014 Dec 15;745:217-22.
Cell experiment: | 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 experiment: | 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: [1]. Fukahori H, et al. Effect of AS2521780, a novel PKCθ selective inhibitor, on T cell-mediated immunity. Eur J Pharmacol. 2014 Dec 15;745:217-22. |
Cas No. | 1214726-89-2 | SDF | |
Canonical SMILES | CSC1=C(CNC2=NC=C(C#N)C(NC[C@@]3(C[C@@H](C4)C5NC[C@H]6CC[C@H](O)CC6)C[C@H]4C[C@H]5C3)=N2)C=CC=N1 | ||
Formula | C30H41N7OS | M.Wt | 547.76 |
الذوبان | Soluble in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 1.8256 mL | 9.1281 mL | 18.2562 mL |
5 mM | 0.3651 mL | 1.8256 mL | 3.6512 mL |
10 mM | 0.1826 mL | 0.9128 mL | 1.8256 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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- Purity: >98.00%
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