Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 987.00 | |
50 mg | 6-8 weeks | $ 1,360.00 | |
100 mg | 6-8 weeks | $ 1,860.00 | |
1 mL * 10 mM (in DMSO) | 6-8 weeks | $ 381.00 |
Description | 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. |
Targets&IC50 | CDK19:4.28 nM, CDK8:0.61 nM, STAT5:, GSK-3α:76.67 nM, GSK-3β:63.06 nM |
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. |
In vivo | 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. |
Molecular Weight | 332.32 |
Formula | C16H12N8O |
CAS No. | 2241300-50-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (752.29 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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AS2863619 free base 2241300-50-3 Cell Cycle/Checkpoint CDK AS-2863619 AS-2863619 free base AS 2863619 AS2863619 inhibitor inhibit