AS2863619 |
| Katalog-Nr.GC38736 |
AS2863619 ermÖglicht die Umwandlung antigenspezifischer Effektor-/GedÄchtnis-T-Zellen in regulatorische Foxp3+-T-Zellen (Treg) zur Behandlung verschiedener immunologischer Erkrankungen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2241300-51-4
Sample solution is provided at 25 µL, 10mM.
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AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene[1].
AS2863619 (1 μM; 22 hours; mouse CD4+ T cells) treatment suppresses serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples[1]. Western Blot Analysis[1] Cell Line: Mouse CD4+ T cells
AS2863619 (30 mg/kg; oral administration; daily; for 2 weeks; mice) treatment after sensitization with 2,4-dinitrofluorobenzene (DNFB) dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of interferon-γ+ (IFN-γ+) cells in a skin contact hypersensitivity model, when compared with vehicle-treated control mice. Treg depletion before the elicitation of the secondary response abolishes AS2863619-induced suppression. KLRG1+ Foxp3+ T cells are specifically increased in DNFB sensitized AS2863619-treated mice[1]. Animal Model: Mice with DNFB-induced contact skin hypersensitivity[1]
[1]. Akamatsu M, et al. Conversion of antigen-specific effector/memory T cells into Foxp3-expressing Treg cells by inhibition of CDK8/19. Sci Immunol. 2019 Oct 25;4(40). pii: eaaw2707.
| Cas No. | 2241300-51-4 | SDF | |
| Canonical SMILES | NC1=NON=C1C(N2C3=CC=C4N=C(C)NC4=C3)=NC5=C2C=CN=C5.[H]Cl.[H]Cl | ||
| Formula | C16H14Cl2N8O | M.Wt | 405.24 |
| Löslichkeit | DMSO: 250 mg/mL (616.92 mM) | 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 | 2.4677 mL | 12.3384 mL | 24.6767 mL |
| 5 mM | 0.4935 mL | 2.4677 mL | 4.9353 mL |
| 10 mM | 0.2468 mL | 1.2338 mL | 2.4677 mL |
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- Purity: >98.00%
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