AS2863619

AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells.

Product information

CAS Number: 2241300-51-4

Molecular Weight: 405.24

Formula: C16H14Cl2N8O

Chemical Name: 4-[1-(2-methyl-1H-1,3-benzodiazol-6-yl)-1H-imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine dihydrochloride

Smiles: Cl.Cl.CC1NC2C=C(C=CC=2N=1)N1C(=NC2C=NC=CC1=2)C1=NON=C1N

InChiKey: LHUAALWRORLTCJ-UHFFFAOYSA-N

InChi: InChI=1S/C16H12N8O.2ClH/c1-8-19-10-3-2-9(6-11(10)20-8)24-13-4-5-18-7-12(13)21-16(24)14-15(17)23-25-22-14;;/h2-7H,1H3,(H2,17,23)(H,19,20);2*1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Solubility (25°C). 60 mg/mL(148.06 mM). 81 mg/mL(199.88 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AS2863619 induction of Foxp3 in vitro does not require exogenous TGF-β. AS2863619-induced iTreg cells can be induced in the presence of inflammatory cytokines such as IL-4, IL-6, and IFN-γ, which appear to hamper Foxp3 gene activation via activation of STATs. AS2863619 is able to generate iTreg cells not only from naïve Tconv cells but also from effector/memory Tconv cells. Furthermore, AS2863619 cannot induce Foxp3 in CDK8 and CDK19 double-deficient T cells. AS2863619-induced iTreg cells require TCR and IL-2 stimulation for their generation and are devoid of Treg-type DNA hypomethylation, which is present in nTreg cells and required for stable Treg function.

In Vivo:

AS2863619 induces in vivo Foxp3 induction in antigen-activated T cells. In vivo AS2863619-induced Foxp3+ T cells are able to gradually acquire Treg-specific epigenetic alterations, differentiating into functionally stable Foxp3+ pTreg cells having a more nTreg-like gene expression profile.

Products are for research use only. Not for human use.