Purdue Bioscience - SpeciPure

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
5 mg	6-8 weeks	$ 339
10 mg	6-8 weeks	$ 610
20 mg	6-8 weeks	$ 901
50 mg	6-8 weeks	$ 1873
100 mg	6-8 weeks	$ 2865

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:, GSK3α:76.67 nM, GSK3β: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.
CAS No.	2241300-50-3
Chemical Formula	C16H12N8O
Molecular Weight	332.327
Solubility	DMSO: 250 mg/mL (752.29 mM), Need ultrasonic
Storage	Powder: -20°C for 2 years In solvent: -80°C for 1 year

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