AS2863619
- Product Name
- AS2863619
- CAS No.
- 2241300-51-4
- Chemical Name
- AS2863619
- Synonyms
- AS2863619;AS2863619, 10 mM in DMSO;Cyclin dependent kinase,AS2863619,STAT,AS 2863619,Inhibitor,inhibit,CDK,AS-2863619;4-(1-(2-Methyl-1H-benzo[d]imidazol-6-yl)-1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine dihydrochloride
- CBNumber
- CB15821249
- Molecular Formula
- C16H13ClN8O
- Formula Weight
- 368.79
- MOL File
- 2241300-51-4.mol
AS2863619 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 10 mM
- form
- A solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- FA176468
- Product name
- AS 2863619
- Packaging
- 1mg
- Price
- $210
- Updated
- 2021/12/16
- Product number
- FA176468
- Product name
- AS 2863619
- Packaging
- 2mg
- Price
- $320
- Updated
- 2021/12/16
- Product number
- 0389EP
- Product name
- 4-[1-(2-Methyl-3H-benzimidazol-5-yl)imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine;dihydrochloride
- Packaging
- 1mg
- Price
- $333
- Updated
- 2021/12/16
- Product number
- CS-0106758
- Product name
- AS2863619
- Purity
- >98.0%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0106758
- Product name
- AS2863619
- Purity
- >98.0%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
AS2863619 Chemical Properties,Usage,Production
Uses
AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene[1].
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[1].
| Animal Model: | Mice with DNFB-induced contact skin hypersensitivity[1] |
| 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. |
IC 50
CDK8: 0.61 nM (IC50); CDK19: 4.28 nM (IC50); GSK3α: 76.67 nM (IC50); GSK3β: 63.06 nM (IC50); STAT5
References
[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. DOI:10.1126/sciimmunol.aaw2707
AS2863619 Preparation Products And Raw materials
Raw materials
Preparation Products
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