BAY-598 : protein-substrate competitive, SAM uncompetitive inhibitor of SMYD2
Protein target names: SMYD2
Mechanism of action: protein-substrate competitive inhibitor, SAM uncompetitive inhibitor
In Vitro Validations
DOI Reference: 10.1021/acs.jmedchem.5b01890
In Cell Validations
In Vivo Data
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SERP ratings and comments
(last updated: 17 May 2016 )
In KYSE-150 cells, BAY-598 reduces p53K370me (relative to p53K370) with IC50 = 50 nM. Use BAY-598 in parallel with its control compound BAY-369 in cell assays.
(last updated: 18 May 2016 )
This is a potent, selective probe suitable for cellular studies with on-target activity expected between 50-1000 nM. If used above 5000 nM, there is a potential for SMYD3 inhibition (unconfirmed). The probe is also suitable for use in vivo in human tumour xenografts in mice with on-target activity expected between 30-100 mg/kg (oral dosing). Full mouse PK, plasma protein binding, and free drug PK-PD relationships in mouse models have not yet been reported. I recommend that the user determine free-drug exposure if dosing above 100 mg/kg (orally) to relate to pharmacology profile. Over the short term (48 h), the compound is chemically stable in standard conditions; racemisation has been observed in basic forcing conditions.
(last updated: 4 Jun 2016 )