AS2863619

CAS No. 2241300-51-4

AS2863619( —— )

Catalog No. M21957 CAS No. 2241300-51-4

AS2863619 is an orally active?inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19 (IC50s of 0.61 nM and 4.28 nM, respectively).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 170 Get Quote
5MG 260 Get Quote
10MG 410 Get Quote
25MG 678 Get Quote
50MG 954 Get Quote
100MG 1287 Get Quote
200MG Get Quote Get Quote
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Biological Information

  • Product Name
    AS2863619
  • Note
    Research use only, not for human use.
  • Brief Description
    AS2863619 is an orally active?inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19 (IC50s of 0.61 nM and 4.28 nM, respectively).
  • Description
    AS2863619 is an orally active?inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19 (IC50s of 0.61 nM and 4.28 nM, respectively).
  • 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. Western Blot Analysis Cell Line:Mouse CD4+ T cells Concentration:1 μM Incubation Time:22 hours Result:Suppressed 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; oral administration; daily; for 2 weeks; mice) treatment after sensitization with 2,4-dinitrofluorobenzene (DNFB) dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of interferon-γ+ (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. Animal Model:Mice with DNFB-induced contact skin hypersensitivity Dosage:30 mg/kg Administration:Oral administration; daily; for 2 weeks Result:The degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreased ratios of interferon-γ+ (IFN-γ+) cells.
  • Synonyms
    ——
  • Pathway
    JAK/STAT Signaling
  • Target
    STAT
  • Recptor
    STAT5|CDK8|CDK19
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2241300-51-4
  • Formula Weight
    405.24
  • Molecular Formula
    C16H14Cl2N8O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:245 mg/ml(604.58 mM; Need ultrasonic)
  • SMILES
    Cl.Cl.Cc1nc2ccc(cc2[nH]1)-n1c(nc2cnccc12)-c1nonc1N
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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