2. PROTAC Immunology/Inflammation
  3. PROTACs IRAK
  4. APH02174

APH02174 is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 blocks inflammatory signals by inhibiting IL-6 release. APH02174 can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis. (Pink: Target Protein Ligand (HY-174470); Blue: CRBN Ligand (HY-45512); Black: Linker; CRBN Ligand+Linker (HY-174796))

For research use only. We do not sell to patients.

APH02174 Chemical Structure

APH02174 Chemical Structure

CAS No. : 3065494-66-5

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APH02174 Related Antibodies

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IRAK1 IRAK4

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Description

APH02174 is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 blocks inflammatory signals by inhibiting IL-6 release. APH02174 can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis. (Pink: Target Protein Ligand (HY-174470); Blue: CRBN Ligand (HY-45512); Black: Linker; CRBN Ligand+Linker (HY-174796)) [1]

IC50 & Target

IRAK4

4.01 nM (DC50)

In Vitro

APH02174 (0.24-1000 nM) can selectively degrade IRAK4 protein in various cells, including THP-1 (DC50 = 4.01 nM), hPBMCs (DC50 = 0.43 nM) and mouse PBMCs (DC50 = 3.57 nM) [1].
APH02174 (0.03-2000 nM; 24 h) significantly inhibits the Lipopolysaccharides (LPS) (HY-D1056) induced IL-6 release in the hPBMCs (IC50 = 16.43 nM) [1].

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

APH02174 Related Antibodies
In Vivo

APH02174 (10-100 mg/kg; twice daily; for 7 days) reduces imiquimod-induced psoriasis-like skin inflammation significantly degrades the IRAK4 protein level in the spleen of the Imiquimod (IMQ) (HY-B0180) induced mice[1].
APH02174 (30 or 100 mg/kg; p.o.; once daily; for 14 days) significantly improves arthritis in the rheumatoid arthritis mice[1].

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

Animal Model: Collagen-induced psoriasis male DBA/1 mice (7 weeks)[1]
Dosage: 30 or 100 mL/kg
Administration: Oral administration (p.o.); once daily for 14 days
Result: Significantly improved arthritis score and reduced inflammation.
Significantly reduced pathological scores and improved pathological structural changes.
Significantly degraded IRAK4 in mouse PBMCs.
Molecular Weight

870.00

Formula

C49H55N7O8
CAS No.
SMILES

OCC1CCN(CC1)C2=CC3=C(C=C2NC(C4=COC5=C4N=CC=C5)=O)CC6(CCN(CC6)C[C@@H]7CC[C@@H](OCC#CC8=C(C(N(C9=O)C%10C(NC(CC%10)=O)=O)=CC=C8)N9C)CC7)O3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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APH02174 Related Classifications

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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:

APH021743065494-66-5APH 02174APH-02174PROTACsIRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseIRAK4PROTACIL-6InflammationInhibitorinhibitorinhibit

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