MS8709

MS8709 : Degrader (PROTAC) of EHMT2, EHMT1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe MS8709 is in the process of SERP review.

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Information

EHMT2
EHMT1

Degrader (PROTAC)

3 uM

Probe Availability:

MedChemExpress

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity of MS8907 (at 10 μM) against a panel of 21 protein methyltransferases was assessed using radioactive methyltransferase assays. EZH2, PRMT7, and SET7/9 were moderately inhibited, but protein levels were not affected but not significantly in 22Rv1 cells treated with MS8907 for 24 h.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

MS8709 was well tolerated at a single IP dose of 50 mg/kg. It is recommended a MTD study is carried out before any repeat dosing efficacy model studies.

(last updated: 13 Jun 2024 )

SERP+ Ratings

In Cell Rating

In Model Organisms

SERP+ Comments:

The probe's selectivity was characterised within the family, but proteome-wide selectivity assessment (global proteomics) is missing. Against three of the 21 tested protein methyltansferases (EZH2, PRMT7, and SET7/9), moderate inhibition was observed, but the probe did not induce their degradation.

(last updated: 6 Feb 2026 )