Activators & Inhibitors

Ezetimibe is an anti-hyperlipidemic medication which is used to lower cholesterol levels. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes.

Ganetespib (also known as STA-9090) is a potent small-molecule inhibitor of heat shock protein 90 (IC50=4 nM). It binds to the ATP pocket in the N-terminus of Hsp90, resulting in down-regulation of Hsp90 client protein levels. Being structurally unrelated to geldanamycin-derived Hsp90 inhibitors (17-AAG, 17-DMAG, and IPI-504), ganetespib has a unique triazolone-containing chemical structure and stands out other Hsp90 inhibitors in terms of potency, antitumor activity, and safety profile.

Ganetespib (also known as STA-9090) is a potent small-molecule inhibitor of heat shock protein 90 (IC50=4 nM). It binds to the ATP pocket in the N-terminus of Hsp90, resulting in down-regulation of Hsp90 client protein levels. Being structurally unrelated to geldanamycin-derived Hsp90 inhibitors (17-AAG, 17-DMAG, and IPI-504), ganetespib has a unique triazolone-containing chemical structure and stands out other Hsp90 inhibitors in terms of potency, antitumor activity, and safety profile.

GSK256066 is a selective PDE4 inhibitor with an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 vs. other PDE isoforms. Often used clinically by inhalation in chronic obstructive pulmonary disease and asthma.

GSK256066 is a selective PDE4 inhibitor with an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 vs. other PDE isoforms. Often used clinically by inhalation in chronic obstructive pulmonary disease and asthma.

CG001 is a small molecule inhibitor that targets Wnt/β-catenin pathway. It inhibits TCF/β-catenin mediated transcription by competing with β-catenin for CBP (CREB binding protein) but not p300 binding with an IC50 of 3 µM. It can be used to specifically evaluate the role of CBP/beta-catenin association on WNT signaling and cell physiology.

CG001 is a small molecule inhibitor that targets Wnt/β-catenin pathway. It inhibits TCF/β-catenin mediated transcription by competing with β-catenin for CBP (CREB binding protein) but not p300 binding with an IC50 of 3 µM. It can be used to specifically evaluate the role of CBP/beta-catenin association on WNT signaling and cell physiology.

CG001 is a small molecule inhibitor that targets Wnt/β-catenin pathway. It inhibits TCF/β-catenin mediated transcription by competing with β-catenin for CBP (CREB binding protein) but not p300 binding with an IC50 of 3 µM. It can be used to specifically evaluate the role of CBP/beta-catenin association on WNT signaling and cell physiology.

Retaspimycin hydrochloride (also known as IPI-504), a hydroquinone hydrochloride salt derivative of 17-AAG, is a novel, potent and selective inhibitor of Hsp90 that binds at the N-terminal ATP/ADP-binding site of Hsp90. Once in the systemic circulation, IPI-504 is deprotonated and converted into the free base IPI-504 which is subsequently oxidized to 17-AAG.