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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.
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.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
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 |
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 | CDK19:4.28 nM, CDK8:0.61 nM, STAT5:, GSK-3α:76.67 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. |
分子量 | 332.32 |
分子式 | C16H12N8O |
CAS No. | 2241300-50-3 |
密度 | 1.75 g/cm3 (Predicted) |
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
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