JH-X-119-01

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

JH-X-119-01  纯度: ≥98.0%

JH-X-119-01 是一种有效的选择性白介素 1 受体相关激酶 1 (IRAK1) 抑制剂。JH-X-119-01 可改善 LPS 诱导的小鼠败血症。JH-X-119-01 抑制 IRAK1，IC50 为 9 nM，而在浓度高达 10 μM 时对 IRAK4 也没有抑制作用。

JH-X-119-01

JH-X-119-01 Chemical Structure

CAS No. : 2227368-54-7

规格 价格 是否有货 数量
5 mg ￥1800 In-stock
10 mg ￥2700 In-stock
25 mg ￥4900 In-stock
50 mg ￥7300 In-stock
100 mg ￥9900 In-stock
200 mg   询价  
500 mg   询价  

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JH-X-119-01 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice[1]. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM[2].

IC50 & Target[2]

IRAK-1

9 nM (IC50)

体外研究
(In Vitro)

JH-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. JH-X-119-01 selectively inhibits IRAK1 phosphorylation[1]. JH-X-119-01 exhibits off-target inhibition of only two additional kinases, YSK4 and MEK3. Dose response analysis reveals an IC50 of 57 nM for YSK4[2]. JH-X-119-01 shows moderate cell killing effects in a panel of Waldenström’s macroglobulinemia (WM) cells, Diffused Large B-cell Lymphoma (DLBCL) cells, and lymphoma cells expressing mutant MYD88, with EC50s ranging from 0.59 to 9.72 μM[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: RAW 264.7 cells and THP-1 cells
Concentration: 10 μM
Incubation Time: 15 minutes
Result: Decreased LPS (100 ng/mL)-induced phosphorylation of IκBα and NF-κB-P65.

体内研究
(In Vivo)

JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (20-22 g, male) mice[1]
Dosage: 5 mg/kg and 10 mg/kg
Administration: Intraperitoneally injected; 5 days
Result: Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg.

分子量

452.46

Formula

C25H20N6O3
CAS 号

2227368-54-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (552.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2101 mL 11.0507 mL 22.1014 mL
5 mM 0.4420 mL 2.2101 mL 4.4203 mL
10 mM 0.2210 mL 1.1051 mL 2.2101 mL

*

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.98 mg/mL (4.38 mM); Clear solution

    此方案可获得 ≥ 1.98 mg/mL (4.38 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 19.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Bin Pan, et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int Immunopharmacol. 2020 Aug;85:106597.

    [2]. John M Hatcher, et al. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243.

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