AH078

AH078 : Degrader (PROTAC) of CSNK1D, CSNK1E

Structure

Information

  • CSNK1D
  • CSNK1E
  • Degrader (PROTAC)
  • 1 µM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): Selectivity within target family: AH078 is not able to degrade CK1a at low concentrations (Dmax 35%) Selectivity of AH078, performed quantitative proteomics analyses was performed using the glioma cell line U-87 and the metastatic breast adenocarcinoma cell line MDA-MB-231 quantifying 9574 and 9777 different protein groups respectively. Only CK1δ and CK1ε, but not CK1α nor any other detected proteins, were significantly reduced, demonstrating exclusive degradation selectivity of AH078 over more than 9000 other proteins that were precisely quantified in both cell lines.
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SERP ratings and comments


No SERP comments found for AH078