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 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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JAK-IN-23

JAK-IN-23 構造式

CAS 番号 : 3031837-35-8

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
5 mg $300 在庫あり
10 mg $480 在庫あり
25 mg $950 在庫あり
50 mg $1450 在庫あり
100 mg $2250 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

JAK-IN-23 関連抗体

Top Publications Citing Use of Products

JAK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
JAK1 JAK2 JAK3 Tyk2 JAK

NF-κB アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

STAT アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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)

Cellular Effect
Cell Line Type Value Description References
HUVEC IC50
> 10 μM
Compound: 8l
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
[PMID: 36053746]
THP1-Dual IC50
150.7 nM
Compound: 8l
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
[PMID: 36053746]
THP1-Dual IC50
3.3 nM
Compound: 8l
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
[PMID: 36053746]
THP1-Dual IC50
4.3 μM
Compound: 8l
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
[PMID: 36053746]
体外実験

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.

JAK-IN-23 関連抗体

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.
体内実験

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].

MedChemExpress (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).
分子量

441.35

分子式

C23H22Cl2N4O
CAS 番号
Appearance

Solid

Color

Light brown to gray

SMILES

OC1=C(Cl)C=C(C2=CC=C3N=CC(N=C(C)N4C5CCN(C)CC5)=C4C3=C2)C=C1Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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)
溶剤 & 溶解度
体外: 

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)

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
View the 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.

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

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 98.88%

COA (255 KB) HNMR (279 KB) LCMS (105 KB)

取扱説明書 (2659 KB)
参考文献

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
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JAK-IN-23 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

JAK-IN-233031837-35-8JAKSTINGNF-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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製品名:
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製品番号:
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