APH02174 hemiformic 

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

APH02174 (0.24-1000 nM) hemiformic 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) hemiformic 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 (10-100 mg/kg; p.o.; twice daily; for 7 days) hemiformic 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 (30-100 mg/kg; p.o.; once daily; for 14 days) hemiformic 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.

916.03

C₄₉H₅₅N₇O₈·1/2CH₂O₂

Solid

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.OC=O.[1/2]

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Wu XW, et al. Discovery of APH02174 as a Highly Selective and Orally Bioavailable IRAK4 Degrader for the Treatment of Inflammatory Diseases. J Med Chem. 2025 Jun 26;68(12):12845-12861.  [Content Brief]