GSK3484862

GSK3484862 : inhibitor of DNMT1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(1 ratings)

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Probe GSK3484862 is in the process of SERP review.

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Information

DNMT1

degrader/inhibitor

up to 1 µM
Reviewer recommended concentration: 80 nM for incubation times >12h

In Vitro Validations

Uniprot ID: P26358

Target Class: Epigenetic

Target SubClass: Methyltransferase

Potency: IC50

Potency Value: 230 nM

Potency Assay: DNMT1 enzymatic inhibition (fluorescent coupled breaklight assay)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

DNA (cytosine-5)-methyltransferase 1, DNMT, CXXC9, ...

DOI Reference: 10.1038/s43018-021-00249-x

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): no inhibition of the family members DNMT3A/3L and DNMT3B/3L, or the assay coupling enzyme Gla1 when tested up to 50 μM

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

GSK3685032 is a potent selective DNMT1 inhibitor that is competitive with the active-site loop of DNMT1 recognition of hemi-methylated DNA. Well characterized for cellular and in vivo activity.

(last updated: 11 Mar 2024 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

GSK3484862 is a selective inhibitor of DNMT1 which displays potent enzymatic and cellular potency. Unlike other DNA hypomethylating agents, GSK348862 is a noncovalent inhibitor which offers the potential for an improved toxicity profile. This probe has been well characterized with co-crystal structures bound to the DNMT1-DNA complex, a multitude of cell-based assays and in vivo efficacy in murine xenograft models. As such, this probe is recommended for biochemical, cell-based and in vivo studies if used at the appropriate concentrations in the respective studies.

(last updated: 5 Apr 2024 )