IRAK4-IN-21
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2170694-04-7
- Formula: C28H28FN7O2
- Molecular Weight:513.57
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Dendritic cell | IC50 |
0.51 μM
Compound: 17
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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
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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
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[PMID: 35450353] |
| HUVEC | IC50 |
0.2 μM
Compound: 17
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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
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[PMID: 35450353] |
| THP-1 | IC50 |
0.17 μM
Compound: 17
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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] |
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.
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Cell Line:THP-1, DC cells (are primed with IFN-γ)
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Concentration:10 µM (a 4-fold serial dilution from 10 µM)
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Incubation Time:1 h (pre-incubate)
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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.
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Cell Line:HUVEC cells (IL-1β-stimulated)
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Concentration:10 µM (a 4-fold serial dilution from 10 µM)
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Incubation Time:1 h (pre-incubate)
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Result:Inhibited the level of IL-6 in the supernatant of HUVEC cells with an IC50 of 0.20 µM.
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Cell Line:Human whole blood (IL-1β-stimulated)
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Concentration:10 µM (a 4-fold serial dilution from 10 µM)
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Incubation Time:1 h (pre-incubate)
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Result:Inhibited the level of MIP-1β in the human whole blood with an IC50 of 0.47 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (acute mouse model; IL-1β-stimulated)[1].
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Dosage:75 mg/kg
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Administration:Oral administration; single (pre-treat).
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Result:Showed 54% inhibition of IL-6, plasma concentrations was 2877 ng/mL at 0.5 h and 496 ng/mL at 2 h.
Chemical Information
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CAS No. 2170694-04-7
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Appearance Solid
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Molecular Weight 513.57
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Formula C28H28FN7O2
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Color White to off-white
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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)=CN=C6)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
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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