AS2863619|2241300-51-4|-陌孚医药/Medlife

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AS2863619

目录号: PL11485 纯度: ≥98.0%

CAS No. :2241300-51-4

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中文名称	AS2863619
英文名称	AS2863619
英文别名	AS2863619;4-(1-(2-methyl-1H-benzo[d]imidazol-6-yl)-1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine 2HCl;4-[1-(2-methyl-1h-benzimidazol-5-yl)-1h-imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine dihydrochloride;4-(1-(2-Methyl-1H-benzo[d]imidazol-6-yl)-1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine dihydrochloride;4-[1-(2-Methyl-3H-benzimidazol-5-yl)imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine;dihydrochlor
Cas No.	2241300-51-4
分子式	C₁₆H₁₄Cl₂N₈O
分子量	405.24
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	AS2863619 可以将抗原特异性效应子/记忆 T 细胞转换为 Foxp3⁺ 调节性 T (T_reg) 细胞，以研究各种免疫疾病。AS2863619 是一种有效的口服的细胞周期蛋白依赖性激酶 8 (CDK8) 和 CDK19 抑制剂，IC₅₀ 分别为 0.61 nM 和 4.28 nM。AS2863619 抑制 CDK8/19 可增强 STAT5 的激活，从而激活 Foxp3 基因。
生物活性	AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 regulatory T (T reg ) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC 50 s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
性状	Solid
IC50 & Target[1][2]	CDK8 0.61 nM (IC50) CDK19 4.28 nM (IC
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis-tbl">
体内研究(In Vivo)	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. T reg 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[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.

溶解度数据	In Vitro: DMSO : 250 mg/mL (616.92 mM; Need ultrasonic)H₂O : ≥ 100 mg/mL (246.77 mM)

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