Dataset Information

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

ABSTRACT: SMYD3 has been implicated in a range of cancers; however, until now no potent selective small molecule inhibitors have been available for target validation studies. A novel oxindole series of SMYD3 inhibitors was identified through screening of the Epizyme proprietary histone methyltransferase-biased library. Potency optimization afforded two tool compounds, sulfonamide EPZ031686 and sulfamide EPZ030456, with cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibition. EPZ031686 shows good bioavailability following oral dosing in mice making it a suitable tool for potential in vivo target validation studies.

SUBMITTER: Mitchell LH

PROVIDER: S-EPMC4753551 | biostudies-literature | 2016 Feb

REPOSITORIES: biostudies-literature

ACCESS DATA

Publications

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Mitchell Lorna H LH Boriack-Sjodin P Ann PA Smith Sherri S Thomenius Michael M Rioux Nathalie N Munchhof Michael M Mills James E JE Klaus Christine C Totman Jennifer J Riera Thomas V TV Raimondi Alejandra A Jacques Suzanne L SL West Kip K Foley Megan M Waters Nigel J NJ Kuntz Kevin W KW Wigle Tim J TJ Scott Margaret Porter MP Copeland Robert A RA Smith Jesse J JJ Chesworth Richard R

ACS medicinal chemistry letters 20150827 2

SMYD3 has been implicated in a range of cancers; however, until now no potent selective small molecule inhibitors have been available for target validation studies. A novel oxindole series of SMYD3 inhibitors was identified through screening of the Epizyme proprietary histone methyltransferase-biased library. Potency optimization afforded two tool compounds, sulfonamide EPZ031686 and sulfamide EPZ030456, with cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibitio ...[more]

PMID: 26985287

Dataset Information

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Publications

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets

Similar Datasets

First-in-human studies of seletalisib, an orally bioavailable small-molecule PI3Kδ inhibitor for the treatment of immune and inflammatory diseases.
| S-EPMC5384962 | biostudies-literature

Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts.
| S-EPMC3386073 | biostudies-literature

A Novel, Orally Bioavailable, Small-Molecule Inhibitor of PCSK9 With Significant Cholesterol-Lowering Properties In Vivo.
| S-EPMC9646673 | biostudies-literature

A SMYD3 Small-Molecule Inhibitor Impairing Cancer Cell Growth.
| S-EPMC4988495 | biostudies-literature

Discovery and Characterization of ZL-2201, a Potent, Highly Selective, and Orally Bioavailable Small-molecule DNA-PK Inhibitor.
| S-EPMC10473160 | biostudies-literature

Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.
| S-EPMC10726352 | biostudies-literature

Discovery of an Orally Bioavailable Small-Molecule Inhibitor for the β-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction.
| S-EPMC8817233 | biostudies-literature

Potent, orally bioavailable diazabicyclic small-molecule mimetics of second mitochondria-derived activator of caspases.
| S-EPMC2679375 | biostudies-literature

Discovery of potent anticancer agent HJC0416, an orally bioavailable small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3).
| S-EPMC4096847 | biostudies-literature

Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor.
| S-EPMC7834599 | biostudies-literature