AS-99
AS-99 : SET non-competitive inhibitor of ASH1L
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
AS-99 is the first selective ASH1L inhibitor and an excellent chemical probe.
(last updated: 29 Jun 2021 )
SERP Ratings
SERP Comments:
The active compound is a thioamide, metabolic to inactive amide may apply dependent on animal model but good PK was shown in this study.
(last updated: 5 Jul 2021 )
SERP Ratings
SERP Comments:
ASH1 is an important epigenetic target. Before this report, there is no high-quality ASH1 inhibitor. AS-99 is the first small-molecular inhibitor of ASH1 with a decent IC50 and promising cellular activity. This compound and its negative control have been well characterized in vitro and in cells regarding the potency, selectivity, and modes of interaction. While the EC50 of AS-99 is modest, this compound has its merit against ASH1 in a cellular context because of the lack of inhibitors against the target. Please note that only the GI50 of AS-99 was reported and its cellular EC50 needs to be evaluated case by case.
(last updated: 6 Jul 2021 )