JAK-IN-23
Based on 1 publication(s) in Google Scholar
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).
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- Pureté : 98.88%
- CAS No.: 3031837-35-8
- Formule: C23H22Cl2N4O
- Masse moléculaire:441.35
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Stockage:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) JAK-IN-23
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Activité biologique
Description
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) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HUVEC | IC50 |
>10 μM
Compound: 8l
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Cytotoxicity against human HUVEC cells assessed as inhibition of cell growth measured after 24 hrs by CCK-8 method
Cytotoxicity against human HUVEC cells assessed as inhibition of cell growth measured after 24 hrs by CCK-8 method
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[PMID: 36053746] |
| THP1-Dual | IC50 |
150.7 nM
Compound: 8l
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Inhibition of LPS induced NF kappa B activation in human THP1-Dual cells stimulated with LPS-B5 for 3 hrs followed by compound addition incubated for 24 hrs
Inhibition of LPS induced NF kappa B activation in human THP1-Dual cells stimulated with LPS-B5 for 3 hrs followed by compound addition incubated for 24 hrs
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[PMID: 36053746] |
| THP1-Dual | IC50 |
3.3 nM
Compound: 8l
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Inhibition of LPS induced ISG activation in human THP1-Dual cells pretreated with LPS-B5 for 3 hrs followed by compound addition incubated for 24 hrs
Inhibition of LPS induced ISG activation in human THP1-Dual cells pretreated with LPS-B5 for 3 hrs followed by compound addition incubated for 24 hrs
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[PMID: 36053746] |
| THP1-Dual | IC50 |
4.3 μM
Compound: 8l
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Cytotoxicity against human THP1-Dual cells assessed as inhibition of cell growth measured after 24 hrs by CCK-8 method
Cytotoxicity against human THP1-Dual cells assessed as inhibition of cell growth measured after 24 hrs by CCK-8 method
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[PMID: 36053746] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP1-Dual Cells
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Concentration:0.33μM, 1μM, 3μM
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Incubation Time:24 h
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS-Induced Acute Colitis Mice Model[1]
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Dosage:1 mg/kg, 3 mg/kg
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Administration:oral
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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).
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Animal Model:The BALB/c mouse inflammatory bowel disease (IBD) model[1]
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Dosage:1 mg/kg, 5 mg/kg
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Administration:oral
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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).
Chemical Information
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CAS No. 3031837-35-8
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Appearance Solid
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Masse moléculaire 441.35
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Formule C23H22Cl2N4O
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Color Light brown to gray
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SMILES
OC1=C(Cl)C=C(C2=CC=C3N=CC(N=C(C)N4C5CCN(C)CC5)=C4C3=C2)C=C1Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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)
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Biophys Res Commun
FATE1: A cancer testis antigen with oncogenic functions - Prognostic biomarker and JAK2/STAT1-driven autophagy regulator in breast cancer. [Abstract]2025 Sep 8:778:152342. PMID: 40737742
Solvant et solubilité
In Vitro:
DMSO : 5 mg/mL (11.33 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (283 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2658 mL | 11.3289 mL | 22.6578 mL | 56.6444 mL |
| 5 mM | 0.4532 mL | 2.2658 mL | 4.5316 mL | 11.3289 mL | |
| 10 mM | 0.2266 mL | 1.1329 mL | 2.2658 mL | 5.6644 mL |
JAK-IN-23 Related Classifications
HY-151262 Related Classifications
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