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.
(Pink: IRAK4 ligand (HY-174470); Blue: Cereblon ligand (HY-45512); Black: linker).
For research use only. We do not sell to patients.
- Formula: C49H55N7O8·1/2CH2O2
- Molecular Weight:916.03
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
|
Cereblon |
IRAK4 |
IL-6 |
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 (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.
Chemical Information
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Appearance Solid
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Molecular Weight 916.03
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Formula C49H55N7O8·1/2CH2O2
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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.OC=O.[1/2]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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