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open-label clinical trial of tasisulam sodium versus paclitaxel as second-line treatment in patients with metastatic melanoma
(2013) Cell 153(7):1552-66
Its affinity to SETD8 was confirmed by ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) studies
Formula: C19H18BrN3O
and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)
IU1 - Proteasome USP14 Inhibitor. CAS# 314245-33-5 size:10mg solid open-label clinical trial of tasisulamIU1, CAS No. 314245 33 5, is a cell permeable, reversible and selective inhibitor of human USP14 with an IC50 of 4. 7 M. It selectively stimulates ubiquitin dependent protein degradation in vitro at 34 M and in MEF cells at 50 M. At 75 M, IU1 reduces accumulation of oxidized proteins in HEK293 cells, alleviating cytotoxicity induced by oxidative stress. Usp14 inhibition accelerated the degradation of oxidized proteins and enhanced resistance to