PROTAC IRAK4 degrader-2
PROTAC IRAK4 degrader-2 is a PROTAC degrader targeting IRAK4. PROTAC IRAK4 degrader-2 induces proteasome-dependent degradation of IRAK4 by recruiting the VHL E3 ligase. PROTAC IRAK4 degrader-2 inhibits multiple cytokines in peripheral blood mononuclear cells. PROTAC IRAK4 degrader-2 can be used in the research of autoimmune diseases, inflammatory diseases and neoplastic diseases.
(Pink: IRAK4 ligand (HY-19836); Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2374122-27-5
- Formula: C57H68FN11O8S
- Molecular Weight:1086.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
IRAK4 |
IL-6 |
IL-8 |
IL-10 |
IL-1β |
TNF-α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PBMC | DC50 |
151 nM
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IRAK4 degradation in human peripheral blood mononuclear cells (PBMCs) assessed by Western blotting after 24 h incubation.
IRAK4 degradation in human peripheral blood mononuclear cells (PBMCs) assessed by Western blotting after 24 h incubation.
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31312412 |
In Vitro
PROTAC IRAK4 degrader-2 (compound 9) (1 nM-10 μM; 24 h or 2 h pretreatment + 22 h) efficiently degrades IRAK4 in human peripheral blood mononuclear cells (PBMCs) via a proteasome-dependent mechanism, with a DC50 of 151 nM[1].
PROTAC IRAK4 degrader-2 (1 nM-1 μM; 24 h) potently degrades IRAK4 in human dermal fibroblasts, with a DC50 of 36 nM[1].
PROTAC IRAK4 degrader-2 (18 h pretreatment + 8 h stimulation) completely inhibits the secretion of multiple proinflammatory cytokines, including IL-6, IL-1β, IFN-γ, IL-8, IL-10 and TNF-α, in human peripheral blood mononuclear cells (PBMCs) stimulated with R848, with pIC50 values ranging from 6.5 to 7.5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PBMC
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Concentration:100 nM, 300 nM, 1 μM, 3 μM, 10 μM
10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM -
Incubation Time:24 h
2 h pretreatment + 22 h -
Result:Degraded IRAK4 in human PBMCs with a DC50 of 151 nM via a proteasome-dependent mechanism.
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Cell Line:human dermal fibroblasts
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Concentration:1 nM, 3 nM, 1 nM, 30 nM, 100 nM, 300 nM, 1 μM
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Incubation Time:24 h
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Result:Induced IRAK4 degradation with a DC50 of 36 nM.
Reduced IRAK4 protein to 4% remaining at 1 μM.
Reduced IRAK4 protein to 9% remaining at 300 nM.
Chemical Information
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CAS No. 2374122-27-5
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Molecular Weight 1086.28
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Formula C57H68FN11O8S
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SMILES
COC1=C(C(N)=O)C=C(C(C#CCN2CCC3(CCN(C4=NC=C(C(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)C=N4)CC3)CC2)=CN=C8OC[C@@H]9[C@H](CC)[C@H](F)C(N9)=O)C8=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC IRAK4 degrader-2 Related Classifications
HY-135382 Related Classifications
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