2. Epigenetics
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Immunology/Inflammation
    NF-κB
  3. JAK
    STING
    NF-κB
    STAT
  4. JAK-IN-23

JAK-IN-23 

Cat. No.: HY-151262 Purity: 98.90%
COA Handling Instructions

JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).

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

JAK-IN-23 Chemical Structure

JAK-IN-23 Chemical Structure

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  • References

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Description

JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD)[1].

IC50 & Target[1]

JAK1

8.9 nM (IC50)

JAK2

15 nM (IC50)

JAK3

46.2 nM (IC50)

NF-κB

150.7 nM (IC50)

ISG

3.3 nM (IC50)

In Vitro

JAK-IN-23 inhibits JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively[1].
JAK-IN-23 shows potent inhibitory activities against ISG and NF-KB with IC50 values of 3.3 nM and 150.7 nM, respectively[1].
WB--- JAK-IN-23 (0.33μM, 1μM, 3μM; 24 h) can simultaneously block JAK-STAT1/3 and NF-κB proinflammatory signaling pathways in THP1-dual cells[1].
JAK-IN-23 (0.003-3 μM; 24 h) decreases the release of various proinflammatory factors, including IL-6, IL-8, IL-1β in THP1-dual cells stimulated by LPS[1].
JAK-IN-23 (0.11-3 μM; 24 h) decreases the release of various proinflammatory factors, including TNF-α, IL-12, IL-10 and IFNγ in LPS-induced peripheral blood mononuclear cells (PBMCs)[1].
JAK-IN-23 (1 μM) inhibits the expression of a variety of inflammation-related genes induced by LPS, including IL-1B, TNF, IL12B, and IL-23A and has inhibitory effects on the expression of genes involved in the unfolded protein response that was induced by LPS (1 μg/mL)[1].

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

Western Blot Analysis[1]

Cell Line: THP1-Dual Cells
Concentration: 0.33μM, 1μM, 3μM
Incubation Time: 24 h
Result: Inhibited p-STAT1/3 in a dose-dependent manner that was induced by IL-6, as well as inhibited pNF-κB p65 in a dose-dependent manner, but not on MYD88 and p-IKK α/β that was induced by LPS.
In Vivo

JAK-IN-23 (1-5 mg/kg, oral) produces a strong anti-inflammatory activity in both dextran sulfate sodium (DSS) - and 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced acute enteritis models and restores the structural composition of gut microbiota[1].

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

Animal Model: DSS-Induced Acute Colitis Mice Model[1]
Dosage: 1 mg/kg, 3 mg/kg
Administration: oral
Result: Significantly decreased the DAI scores (1 and 3 mg/kg).
Recovered the length of the colon (3 mg/kg).
Significantly reduced the histopathology of ulcerative colitis (1 and 3 mg/kg).
Animal Model: The BALB/c mouse inflammatory bowel disease (IBD) model[1]
Dosage: 1 mg/kg, 5 mg/kg
Administration: oral
Result: Significantly improved the survival probability, had low DAI scores and effectively relieved symptoms of colitis in the TNBS-induced IBD mice model (5 mg/kg).
Did not improve the survival probability and decreases the DAI score (100 mg/kg).
Molecular Weight

441.35

Appearance

Solid

Formula

C23H22Cl2N4O
SMILES

OC1=C(Cl)C=C(C2=CC=C3N=CC(N=C(C)N4C5CCN(C)CC5)=C4C3=C2)C=C1Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (11.33 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2658 mL 11.3289 mL 22.6578 mL
5 mM 0.4532 mL 2.2658 mL 4.5316 mL
10 mM 0.2266 mL 1.1329 mL 2.2658 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

JAK-IN-23JAKSTINGNF-κBSTATJanus kinaseStimulator of Interferon GenesTMEM173MITAERISMPYSNuclear factor-κBNuclear factor-kappaBJAK1/2/3JAK/STATinterferon-stimulated genes (ISG)anti-inflammatoryproinflammatory factorsIL-6IL-8IL-1βTNF-aIL-12IFNγinflammatory bowel disease (IBD)Inhibitorinhibitorinhibit

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