AS2863619 | CDK8/19 inhibitor, Foxp3 inducer | Probechem Biochemicals

Chemical Structure : AS2863619

CAS No.: 2241300-51-4

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AS2863619 (AS-2863619)

货号: PC-24914Not For Human Use, Lab Use Only.

AS2863619 is a potent, selective and orally active inhibitor of CDK8 and CDK19 with IC50 of 0.61 nM and 4.28 nM, respectively, AS2863619 is a potent Foxp3 inducer in Tconv cells with EC50 of 32.5 nM.

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5 mg	￥2380	In stock
10 mg	￥3880	In stock
25 mg	￥5980	In stock
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100 mg		Get quote

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生物&药学活性

AS2863619 is a potent, selective and orally active inhibitor of CDK8 and CDK19 with IC50 of 0.61 nM and 4.28 nM, respectively, AS2863619 is a potent Foxp3 inducer in Tconv cells with EC50 of 32.5 nM.
AS2863619 could generate Foxp3+ T cells from naïve Foxp3−CD4+ Tconv cells in a dose-dependent fashion, also substantially enhances FOXP3 expression in human CD4+ and CD8+ Tconv cells in the peripheral blood.
AS2863619 does not exhibit cellular toxicity or hinder proliferative activity of Tconv cells in the concentration range having Foxp3-inducing activity.
AS2863619 inhibits the ability of activated CDK8/19 to phosphorylate the serine residue in the PSP motif of STAT5, augments the retention of the tyrosine-phosphorylated STAT5 in the nucleus, leading to enhanced activation of STAT5, which consequently activates the Foxp3 gene.
AS2863619 (30 mg/kg) induced Foxp3 in KJ1-26+ T cells in DO11.10 TCR transgenic mice, effectively suppressed skin contact hypersensitivity and autoimmune disease in animal models.

物理化学性质&存储条件

分子量	405.24
分子式	C16H14Cl2N8O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Wang L, et al. Mater Today Bio. 2023 Jan 20;19:100557.

2. Akamatsu M, et al. Sci Immunol. 2019 Oct 25;4(40):eaaw2707.

AS2863619 (AS-2863619)

生物&药学活性

物理化学性质&存储条件

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AS2863619 (AS-2863619)

生物&药学活性

物理化学性质&存储条件

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