Highly selective and potent (IC50 90 nM) non covalent inhibitor of USP7
XL188 is a highly selective and potent (IC50 90 nM) non covalent inhibitor of USP7 that binds to the USP7 active site. XL188 facilitates degradation of HDM2, and increases the levels of p53 and p21 in MCF7 cells.
Cell chemical biology, 24(12), 1490-1500 (2017-10-24)
Deubiquitinating enzymes (DUBs) have garnered significant attention as drug targets in the last 5-10 years. The excitement stems in large part from the powerful ability of DUB inhibitors to promote degradation of oncogenic proteins, especially proteins that are challenging to
The Journal of experimental medicine, 215(8), 2137-2155 (2018-07-27)
Ewing sarcoma is a pediatric cancer driven by EWS-ETS transcription factor fusion oncoproteins in an otherwise stable genomic background. The majority of tumors express wild-type TP53, and thus, therapies targeting the p53 pathway would benefit most patients. To discover targets
Deubiquitinating enzymes (DUBs) catalyze the removal of ubiquitin, thereby reversing the activity of E3 ubiquitin ligases and are central to the control of protein abundance and function. Despite the growing interest in DUBs as therapeutic targets, cellular functions for DUBs
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