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AS2863619

Catalog No.GC38736

AS2863619는 다양한 면역 질환 치료를 위해 항원 특이적 효과기/기억 T 세포를 Foxp3+ 조절 T(Treg) 세포로 전환할 수 있습니다.

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AS2863619 Chemical Structure

Cas No.: 2241300-51-4

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$249.00
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5mg
US$279.00
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10mg
US$441.00
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50mg
US$1,323.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

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
Solubility 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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리뷰

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Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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