Cat. No.: HY-126675A

AS2863619

6 Cited Publications

Customer Review

Based on 6 publication(s) in Google Scholar

AS2863619 is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 targets Stat5a-CDK8/19 to promote the differentiation of CD4⁺ T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 can be applied to research in related fields such as periodontitis-induced bone defects.

For research use only. We do not sell to patients.

Purity: 98.02%
CAS No.: 2241300-51-4
Formula: C₁₆H₁₄Cl₂N₈O
Molecular Weight:405.24

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

AS2863619 Chemical Structure

CAS No.: 2241300-51-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

CDK8

0.61 nM (IC₅₀)

CDK19

4.28 nM (IC₅₀)

GSK3α

76.67 nM (IC₅₀)

GSK3β

63.06 nM (IC₅₀)

STAT5

All STAT Isoforms :

All CDK Isoforms :

All TGF-beta/Smad Isoforms :

Smad1
Smad3

In Vitro

AS2863619 , combination with IL-2 and TGF-β, enhances the differentiation of primary CD4+ T cells isolated from the spleens of DBA/1 mice into Treg, and its efficacy is superior to that of the regimens using IL-2 alone combined with either TGF-β or AS2863619^[1].
AS2863619 (125 nM-2 μM; 7-10 d) enhances osteogenic differentiation of human periodontal ligament stem cells, with concentrations of 250 nM and 500 nM increasing ALP activity, upregulating key osteogenic markers, and accelerating mineralized nodule formation on day 10^[2].
AS2863619 (250 nM-500 nM; 7-21 d) inhibits adipogenic differentiation of human periodontal ligament stem cells by reducing lipid droplet formation and downregulating key adipogenic genes^[2].
AS2863619 (250 nM-500 nM; 7-10 d) alleviates rhTNF-α-induced osteogenic differentiation impairment of human periodontal ligament stem cells by inhibiting the RIG-I/MDA5 receptor-mediated RLR signaling pathway, and the 500 nM concentration reverses the inflammatory impairment blocked by the RLR agonist Poly (I:C)^[2].
Combination of AS2863619 (1 mM/mL; 5 d) with IL-2 and TGF-β₁ induces transdifferentiation of allogeneic antigen-specific Balb/c CD4⁺ T cells into ag-Treg, while upregulating the expression of Treg-specific genes and enriching pathways associated with T cell tolerance induction^[3].
AS2863619 (0.01-10 μM; 2 h) significantly increases the apoptosis level of human polymorphonuclear neutrophils (PMNs) stimulated by IC, with a value comparable to that of the negative control group, while it does not significantly reduce cell viability^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

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. T_reg 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^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 2241300-51-4
Appearance Solid
Molecular Weight 405.24
Formula C₁₆H₁₄Cl₂N₈O
Color White to off-white
SMILES

NC1=NON=C1C(N2C3=CC=C4N=C(C)NC4=C3)=NC5=C2C=CN=C5.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (6)

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Cell Stem Cell

Human iPSC-derived CD4+ Treg-like cells engineered with chimeric antigen receptors control GvHD in a xenograft model. [Abstract]

2024 Jun 6;31(6):795-802.e6. PMID: 38848686
Biomaterials

Engineered peripheral CD4 T cells delivery across the BBB promote intracerebral Treg conversion unleashes microglial phagocytotic activity for Alzheimer's disease treatment. [Abstract]

2026 Feb:325:123574. PMID: 40763582
JCI Insight

CAR-engineered cytolytic Tregs reverse pulmonary fibrosis and remodel the fibrotic niche with limited CRS. [Abstract]

2025 Jul 8;10(15):e182050. PMID: 40627450
bioRxiv

2025 Nov 20.
Patent

US20250230411A1.
Elife

Sustained store-operated calcium entry utilizing activated chromatin state leads to instability in iTregs. [Abstract]

2023 Dec 6:12:RP88874. PMID: 38055613

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (616.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 100 mg/mL (246.77 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4677 mL

12.3384 mL

24.6767 mL

5 mM

0.4935 mL

2.4677 mL

4.9353 mL

10 mM

0.2468 mL

1.2338 mL

2.4677 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.62 mg/mL (6.47 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.62 mg/mL (6.47 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.25 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.25 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.25 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (291 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Fang K, et al. Progress and Future Perspectives of Treg Cell Therapy. Front Biosci (Landmark Ed). 2025;30(11):41250. [Content Brief]

[2]. He H, et al. AS2863619 boosts osteogenesis in periodontal ligament stem cells and mitigates inflammatory impairment. Int Immunopharmacol. 2025;161:115101. [Content Brief]

[3]. Bulygin A, et al. Assessment and Characterization of Induced Alloantigen-Specific Regulatory T Cells Obtained by the Inhibition of CDK8/19 with the AS2863619 Compound. Int J Mol Sci. 2025;26(22):10957. Published 2025 Nov 12. [Content Brief]

[4]. Schlotfeldt M, et al. CDK7, CDK9, or CDK11 Inhibition Reduces Neutrophil-Driven Inflammation and Tissue Damage in Experimental Autoimmune Models[J]. bioRxiv, 2025: 2025.11. 19.689221.

[5]. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.4677 mL	12.3384 mL	24.6767 mL	61.6918 mL
	5 mM	0.4935 mL	2.4677 mL	4.9353 mL	12.3384 mL
	10 mM	0.2468 mL	1.2338 mL	2.4677 mL	6.1692 mL
	15 mM	0.1645 mL	0.8226 mL	1.6451 mL	4.1128 mL
	20 mM	0.1234 mL	0.6169 mL	1.2338 mL	3.0846 mL
	25 mM	0.0987 mL	0.4935 mL	0.9871 mL	2.4677 mL
	30 mM	0.0823 mL	0.4113 mL	0.8226 mL	2.0564 mL
	40 mM	0.0617 mL	0.3085 mL	0.6169 mL	1.5423 mL
	50 mM	0.0494 mL	0.2468 mL	0.4935 mL	1.2338 mL
	60 mM	0.0411 mL	0.2056 mL	0.4113 mL	1.0282 mL
	80 mM	0.0308 mL	0.1542 mL	0.3085 mL	0.7711 mL
	100 mM	0.0247 mL	0.1234 mL	0.2468 mL	0.6169 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

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AS2863619

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) AS2863619

All STAT Isoforms

All CDK Isoforms

All TGF-beta/Smad Isoforms

Biological Activity

Chemical Information

Publications (6)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AS2863619 Related Classifications

HY-126675A Related Classifications