APH02174

APH02174 : Degrader (PROTAC) of IRAK4

Structure

Information

  • IRAK4
  • Degrader (PROTAC)
  • up to 100 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): The degradative selectivity of APH02174 was evaluated using tandem mass tag-based global discovery proteomics. After being treated with 300 nM APH02174 for 24 h, IRAK4 was the most degraded protein (>200-fold than other proteins, among approximately 8000 total proteins) in hPBMCs.
Potency assay, off target (cells): To determine whether APH02174 can degrade the transcription factor SALL4 and Zn-finger proteins (IKZF1, IKZF3), WB assays in hPBMCs were conducted, and the degradation of these targets was not observed at the highest testing concentration, 1 μM.
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SERP ratings and comments


No SERP comments found for APH02174