A-196
Substrate-competitive inhibitor, SAM non-competitive inhibitor of KMT5B, KMT5C
Structure
In Cells
In Model Organisms
Information
Protein target names: KMT5B, KMT5C
Mechanism of action: Substrate-competitive inhibitor, SAM non-competitive inhibitor
In Vitro Validations
DOI Reference: 10.1038/nchembio.2282
In Cell Validations
In Vivo Data
No in Vivo Validations
Reagent authentication certificate:
SERP ratings and comments
SERP Ratings
(last updated: 15 Mar 2017 )
SERP Ratings
(last updated: 21 Mar 2017 )
SERP Ratings
SERP Comments:
This probe represents the best in class for SUV420H1 and H2 - hitting the enzymes at 25 and 144 nM, respectively, with selectivity data against a wide panel of related epigenetic and other targets. The originating paper gives good confidence around this molecule and includes strong biochemical, biophysical, structural & cellular data, as well as structurally related negative controls. No data are presented for the wider pharmacokinetic, drug-like profiles, and so no conclusion can be drawn on its suitability as a probe for use in model organism studies. However, permeability from cellular studies and chemical structure would support its further investigation towards these studies.
(last updated: 30 Mar 2017 )