AS2863619 free base

AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.

产品编号 T10382Cas号 2241300-50-3

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AS2863619 free base

产品编号 T10382Cas号 2241300-50-3

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规格	价格	库存
2 mg	¥ 1,730	5日内发货
5 mg	¥ 2,690	5日内发货
25 mg	¥ 9,390	6-8周
50 mg	¥ 12,200	6-8周
100 mg	¥ 17,500	6-8周
1 mL x 10 mM (in DMSO)	¥ 2,830	5日内发货

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产品介绍

生物活性

产品描述	AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
靶点活性	GSK-3α:76.67 nM, STAT5:, CDK8:0.61 nM, CDK19:4.28 nM, GSK-3β:63.06 nM
体外活性	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.
体内活性	AS2863619 (30 mg/kg; p.o.; daily; for 2 weeks; mice) treatment after sensitization with DNFB dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of 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.

化学信息

分子量	332.32
分子式	C₁₆H₁₂N₈O
CAS No.	2241300-50-3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 250 mg/mL (752.29 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0091 mL	15.0457 mL	30.0915 mL	150.4574 mL
5 mM	0.6018 mL	3.0091 mL	6.0183 mL	30.0915 mL
10 mM	0.3009 mL	1.5046 mL	3.0091 mL	15.0457 mL
20 mM	0.1505 mL	0.7523 mL	1.5046 mL	7.5229 mL
50 mM	0.0602 mL	0.3009 mL	0.6018 mL	3.0091 mL
100 mM	0.0301 mL	0.1505 mL	0.3009 mL	1.5046 mL