IRAK4-IN-22
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 99.44%
- CAS No.: 2170694-05-8
- 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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Dendritic cell | IC50 |
0.11 μM
Compound: 18
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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
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[PMID: 35450353] |
| HUVEC | IC50 |
0.11 μM
Compound: 18
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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] |
| HUVEC | IC50 |
0.12 μM
Compound: 18
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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] |
| THP-1 | IC50 |
0.1 μM
Compound: 18
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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
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[PMID: 35450353] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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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 0.10 and 0.11 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 0.11 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 0.51 µM.
In Vivo
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 64% inhibition of IL-6, plasma concentrations was 6817 ng/mL at 0.5 h and 700 ng/mL at 2 h.
Chemical Information
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CAS No. 2170694-05-8
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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)=NC=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
In Vitro:
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)
Protocols
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Imiquimod-Induced Psoriasiform Dermatitis
Imiquimod (IMQ)-induced psoriasiform dermatitis is a widely used murine model in which topical application of IMQ, a Toll-like receptor 7 (TLR7) agonist, triggers innate immune activation in the skin and induces a psoriasis-like inflammatory cascade characterized by epidermal hyperplasia, immune cell infiltration, and cytokine production dominated by the IL-23/IL-17 axis. This inflammatory response is mediated through activation of dendritic cells and downstream induction of IL-23, IL-17A, IL-22, and related pro-inflammatory mediators, recapitulating key features of human plaque psoriasis and enabling mechanistic and therapeutic studies. The model is commonly induced using Aldara (5% IMQ cream) applied topically to murine skin, resulting in rapid onset of erythema, scaling, and thickening that can be quantified as disease severity indices and validated histologically.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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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