2. Immunology/Inflammation
  3. IRAK
  4. IRAK4-IN-21

IRAK4-IN-21 (化合物 17) 是一种口服有效的和具有选择性的强效 IRAK4 抑制剂，其对 IRAK4 和 TAK1 的 IC50 值分别为 5 和 56 nM。IRAK4-IN-21 能够有效抑制 IL-23 的产生 (IC50=0.17 µM)，可用于自身免疫性疾病，如斑块状银屑病和银屑病关节炎的研究。

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IRAK4-IN-21 Chemical Structure

IRAK4-IN-21 Chemical Structure

CAS No. : 2170694-04-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5423
In-stock
1 mg ￥2181
In-stock
5 mg ￥4800
In-stock
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IRAK4-IN-21 相关抗体

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IRAK1 IRAK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Dendritic cell IC50
0.51 μM
Compound: 17
Antiinflammatory activity against human monocyte derived dendritic cells assessed as inhibition of LPS induced IL-23 production preincubated with compound for 1 hr followed by LPS stimulation and measured after 18 hrs by cell based ELISA method
Antiinflammatory activity against human monocyte derived dendritic cells assessed as inhibition of LPS induced IL-23 production preincubated with compound for 1 hr followed by LPS stimulation and measured after 18 hrs by cell based ELISA method
[PMID: 35450353]
HUVEC IC50
0.18 μM
Compound: 17
Antiinflammatory activity against HUVEC cells assessed as inhibition of LPS induced IL-6 production measured by ELISA method
Antiinflammatory activity against HUVEC cells assessed as inhibition of LPS induced IL-6 production measured by ELISA method
[PMID: 35450353]
HUVEC IC50
0.2 μM
Compound: 17
Antiinflammatory activity against HUVEC cells assessed as inhibition of IL-1beta induced IL-6 production preincubated with compound for 1 hr followed by IL-1beta stimulation and measured after 12 hrs by cell based ELISA method
Antiinflammatory activity against HUVEC cells assessed as inhibition of IL-1beta induced IL-6 production preincubated with compound for 1 hr followed by IL-1beta stimulation and measured after 12 hrs by cell based ELISA method
[PMID: 35450353]
THP-1 IC50
0.17 μM
Compound: 17
Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS induced IL-23 production preincubated with compound for 1 hr followed by LPS stimulation and measured after 18 hrs by cell based ELISA method
Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS induced IL-23 production preincubated with compound for 1 hr followed by LPS stimulation and measured after 18 hrs by cell based ELISA method
[PMID: 35450353]
体外研究
(In Vitro)

IRAK4-IN-21 (a 4-fold serial dilution from 10 µM; 1 h) decreases the levels of IL-23 (in THP-1 and DC cells), IL-6 (in HUVEC cells) and MIP-1β (in human whole blood)[1].

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

IRAK4-IN-21 相关抗体:

Cell Viability Assay[1]

Cell Line: THP-1, DC cells (are primed with IFN-γ)
Concentration: 10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time: 1 h (pre-incubate)
Result: Inhibited the levels of IL-23 in the supernatant of THP-1 and DC cells with IC50 of 0.17 and 0.51 µM, respectively.

Cell Viability Assay[1]

Cell Line: HUVEC cells (IL-1β-stimulated)
Concentration: 10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time: 1 h (pre-incubate)
Result: Inhibited the level of IL-6 in the supernatant of HUVEC cells with an IC50 of 0.20 µM.

Cell Viability Assay[1]

Cell Line: Human whole blood (IL-1β-stimulated)
Concentration: 10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time: 1 h (pre-incubate)
Result: Inhibited the level of MIP-1β in the human whole blood with an IC50 of 0.47 µM.
体内研究
(In Vivo)

IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production[1].

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

Animal Model: BALB/c mice (acute mouse model; IL-1β-stimulated)[1].
Dosage: 75 mg/kg
Administration: Oral administration; single (pre-treat).
Result: Showed 54% inhibition of IL-6, plasma concentrations was 2877 ng/mL at 0.5 h and 496 ng/mL at 2 h.
分子量

513.57

Formula

C28H28FN7O2
CAS 号
性状

固体

颜色

White to off-white

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
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (194.72 mM; 超声助溶; 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 1.9472 mL 9.7358 mL 19.4715 mL
5 mM 0.3894 mL 1.9472 mL 3.8943 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。-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

只
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

IRAK4-IN-21 相关分类

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。-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 1.9472 mL 9.7358 mL 19.4715 mL 48.6789 mL
5 mM 0.3894 mL 1.9472 mL 3.8943 mL 9.7358 mL
10 mM 0.1947 mL 0.9736 mL 1.9472 mL 4.8679 mL
15 mM 0.1298 mL 0.6491 mL 1.2981 mL 3.2453 mL
20 mM 0.0974 mL 0.4868 mL 0.9736 mL 2.4339 mL
25 mM 0.0779 mL 0.3894 mL 0.7789 mL 1.9472 mL
30 mM 0.0649 mL 0.3245 mL 0.6491 mL 1.6226 mL
40 mM 0.0487 mL 0.2434 mL 0.4868 mL 1.2170 mL
50 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9736 mL
60 mM 0.0325 mL 0.1623 mL 0.3245 mL 0.8113 mL
80 mM 0.0243 mL 0.1217 mL 0.2434 mL 0.6085 mL
100 mM 0.0195 mL 0.0974 mL 0.1947 mL 0.4868 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.

Keywords:

IRAK4-IN-212170694-04-7IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseplaque psoriasispsoriatic arthritisTHP-1DCHUVECInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-151363
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