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AS2863619 free base

Catalog No. T10382   CAS 2241300-50-3

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.

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AS2863619 free base Chemical Structure
AS2863619 free base, CAS 2241300-50-3
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
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

TargetMolReferences and Literature

1. Akamatsu M, et al. Conversion of antigen-specific effector/memory T cells into Foxp3-expressing Treg cells by inhibition of CDK8/19. Sci Immunol. 2019 Oct 25;4(40). pii: eaaw2707.

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Keywords

AS2863619 free base 2241300-50-3 Cell Cycle/Checkpoint CDK AS-2863619 AS-2863619 free base AS 2863619 AS2863619 inhibitor inhibit

 

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