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

JAK-IN-23 是 JAK/STAT 和 NF-κB 的双重抑制剂,具有口服活性。JAK-IN-23 对J AK1/2/3 具有抑制作用,IC50 值分别为 8.9 nM、15 nM 和 46.2 nM。JAK-IN-23 对干扰素刺激基因 (ISG) 和 NF-κB 通路具有较强的抑制活性,IC50 值分别为 3.3 nM 和 150.7 nM。JAK-IN-23 具有很强的抗炎作用,可以减少各种促炎因子的释放。JAK-IN-23 可用于炎症性肠病 (IBD) 的研究。

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JAK-IN-23 Chemical Structure

JAK-IN-23 Chemical Structure

CAS No. : 3031837-35-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

细胞效力
(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]
体外研究
(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.
体内研究
(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).
分子量

441.35

Formula

C23H22Cl2N4O

CAS 号
性状

固体

颜色

Light brown to gray

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 5 mg/mL (11.33 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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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产品名称:
JAK-IN-23
目录号:
HY-151262
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