2. Immunology/Inflammation
  3. IRAK
  4. IRAK4-IN-22

IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis.

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IRAK4-IN-22

IRAK4-IN-22 構造式

CAS 番号 : 2170694-05-8

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  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 452 在庫あり
Solution
10 mM * 1 mL in DMSO USD 452 在庫あり
Solid
5 mg $400 在庫あり
10 mg $680 在庫あり
25 mg $1350 在庫あり
50 mg $2200 在庫あり
100 mg $3400 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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IRAK4-IN-22 関連抗体

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IRAK 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
IRAK1 IRAK3 IRAK4

  • 生物活性

  • 純度とドキュメンテーション

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製品説明

IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].

Cellular Effect
Cell Line Type Value Description References
Dendritic cell IC50
0.11 3
Compound: 18
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]
Dendritic cell IC50
0.11 3
Compound: 18
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]
Dendritic cell IC50
0.11 3
Compound: 18
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
0.11 3
Compound: 18
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]
HUVEC IC50
0.11 3
Compound: 18
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]
HUVEC IC50
0.11 3
Compound: 18
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]
HUVEC IC50
0.12 3
Compound: 18
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
0.12 3
Compound: 18
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
0.12 3
Compound: 18
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]
THP-1 IC50
0.1 3
Compound: 18
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]
THP-1 IC50
0.1 3
Compound: 18
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]
THP-1 IC50
0.1 3
Compound: 18
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]
体外実験

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].

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

IRAK4-IN-22 関連抗体

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 0.10 and 0.11 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 0.11 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 0.51 µM.
体内実験

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].

MedChemExpress (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 64% inhibition of IL-6, plasma concentrations was 6817 ng/mL at 0.5 h and 700 ng/mL at 2 h.
分子量

513.57

分子式

C28H28FN7O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1[C@@H](C2)C=C[C@@H]2[C@H]1NC3=NC(NC4=CC=CC(C(N5CCCC5)=O)=C4)=NC=C3C6=CC(F)=NC=C6)N
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (194.72 mM; Need ultrasonic; 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 1.9472 mL 9.7358 mL 19.4715 mL
5 mM 0.3894 mL 1.9472 mL 3.8943 mL
10 mM 0.1947 mL 0.9736 mL 1.9472 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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一般には略語で表示されます：C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション
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. 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 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
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IRAK4-IN-22 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:

IRAK4-IN-222170694-05-8IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseplaque psoriasispsoriatic arthritisTHP-1DCHUVECInhibitorinhibitorinhibit

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製品名:
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製品番号:
HY-151365
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