Formulation: A solid
Formal Name: rel-(4R,5R)-4,5-dihydro-2-(4-methoxyphenyl)-4-phenyl-1-(phenylmethyl)-5-[4-[(phenylmethyl)amino]phenyl]-1H-imidazole-4-carboxylic acid, ethyl ester
Purity: ≥98%
Formula Markup: C39H37N3O3
Formula Weight: 595,7
Shelf life (days): 1460
CAS Number: 1446350-60-2
Notes: TCH-165 is a modulator of proteasome assembly.{67664} It selectively activates the chymotrypsin-like, trypsin-like, and caspase-like activities of the 20S proteasome (EC50s = 4.2, 3.2, and 4.7 µM, respectively) over the same activities of the 26S proteasome (EC50s = >70 µM for all) but also inhibits the chymotrypsin-like activity of the 20S proteasome (IC50 = 1.44 µM) in cell-free assays.{67664,67665} TCH-165 (10 µM) increases the 20S proteasome-dependent degradation of the intrinsically disordered proteins α-synuclein and tau.{67664} It enhances disassembly of the 26S proteasome with a concomitant increase in 20S proteasome levels in HEK293T cells in a time-and concentration-dependent manner. TCH-165 (100 mg/kg, p.o.) decreases tumor volume in an RPMI-8226 multiple myeloma mouse xenograft model.{67666} It decreases infarct volume as a percentage of the area at risk in a mouse model of cardiac ischemia-reperfusion injury induced by left anterior descending coronary artery occlusion when administered at a dose of 50 mg/kg.{67667}
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