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Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen
and potential for combination in preclinical models
At 5 μM it directly inhibits DUB activity of USP9x
Smiles: NCC(CS(O)(=O)=O)C1C=CC(Cl)=CC=1
When Delpazolid (LCB-0371) is administered at 100 mg/kg daily (by gavage)
MGCD0103 - CAS# 726169-73-9 Catalog No.:M6555-10 Identification of small molecule inhibitorsMGCD0103, also known as Mocetinostat, CAS No. 726169 73 9, is a rationally designed, orally available, Class 1 selective, small molecule, 2 aminobenzamide HDAC inhibitor with potential antineoplastic activity. MGCD0103 binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur
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