MS8709

MS8709 : Degrader (PROTAC) of EHMT2, EHMT1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe MS8709 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

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.

I have extra information to add

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 )