PTPN1-Degrader-75

PTPN1-Degrader-75 : Degrader (PROTAC) of PTPN1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe PTPN1-Degrader-75 is in the process of SERP review.

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Information

PTPN1

Degrader (PROTAC)

up to 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): Several PTP members including PTP1B, SHP1, SHP2, LYP, and CD45 were tested for their degradation efficacy by treatment of 250 nM and 500 nM compound 75 for 24 h using HepG2 cells. Cpd 75 could lead to mostly complete removal of PTP1B, whereas other PTP members were not found any appreciable degradation except weak reduction of CD45.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

PROTAC 75 has been characterised only in cell-based assays. It shows reasonable target degradation across a range of concentrations with no evidence of a Hook effect. There is evidence that the degradation is selective and due to the ubiquitin proteasome system. The precursor Oleanolic acid is a weak inhibitor and the evidence that conversion into the PROTAC has maintained or improved binding is limited. Overall the evidence for target degradation is reasonable but the probe is not fully mechanistically characterised and is based on a scaffold likely to have other biological effects and so should be used with caution.

(last updated: 1 Sept 2024 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Proteomic profiling would be necessary to fully evaluate this compounds' selectivity.

(last updated: 31 Oct 2024 )