GNE-049
Inhibitor of CREBBP, EP300
Structure
In Cells
In Model Organisms
Probe GNE-049 is in the process of SERP review.
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SERP ratings and comments
SERP Ratings
SERP Comments:
GNE-049 has been studied in various cellular assays and is a potent, selective, cell-penetrant probe. It has also been evaluated in preliminary PK studies in 4 species (mouse, rat, dog, cyno) and studied in preliminary high dose rat TK up to 250 mg/kg, at which dose adverse CNS-related signs were observed. Kpuu 3h post dose was 0.43. A second probe, GNE-781 (cpd 19 in the same paper) has a similar profile to GNE-049, but with higher polar surface area and no CNS penetration. Both probes are high quality, the 2nd probe GNE-781 has more published in vivo data, and unless there is a need for CNS penetration, then should be used in preference to this probe GNE-049. However, both are high quality probes.
(last updated: 24 Mar 2021 )