Activators & Inhibitors

AT13387, discovered by a high-throughput x-ray craystallography fragment-based platform, is a non-geldanamycin inhibitor of heat shock proterin 90 (HPS90), a molecule chaperone regulating signal transduction pathways for cell growth and survival. It has high affinity for binding HSP90 (Kd = 0.5nM) and exhibited an in vitro cytotoxicity showing a median EC50 value of 41 nM. The antitumor activity of AT13387 against solid tumor and leukemia models is similar to alvespimycin.

Bendamustine HCl is an alkylating agent associated with DNA damage (IC50 = 50 µM). It is a cytostatic agent that displays activity in non-Hodgkin's lymphomas.

Bendamustine HCl is an alkylating agent associated with DNA damage (IC50 = 50 µM). It is a cytostatic agent that displays activity in non-Hodgkin's lymphomas.

Betulinic acid is a natural pentacyclic triterpenoid that selectively induces apoptosis in tumor cells by directly activating the mitochondrial pathway of apoptosis through a p53- and CD95-independent mechanism. Betulinic acid also displays TGR5 agonist activity (EC50 =1.04 µM). Betulinic acid is used to study its potential cardiovascular role in the modulation of endothelium-dependent relaxation. Betulinic acid displays anti-HIV and antitumor activity.

Betulinic acid is a natural pentacyclic triterpenoid that selectively induces apoptosis in tumor cells by directly activating the mitochondrial pathway of apoptosis through a p53- and CD95-independent mechanism. Betulinic acid also displays TGR5 agonist activity (EC50 =1.04 µM). Betulinic acid is used to study its potential cardiovascular role in the modulation of endothelium-dependent relaxation. Betulinic acid displays anti-HIV and antitumor activity.

Betulinic acid is a natural pentacyclic triterpenoid that selectively induces apoptosis in tumor cells by directly activating the mitochondrial pathway of apoptosis through a p53- and CD95-independent mechanism. Betulinic acid also displays TGR5 agonist activity (EC50 =1.04 µM). Betulinic acid is used to study its potential cardiovascular role in the modulation of endothelium-dependent relaxation. Betulinic acid displays anti-HIV and antitumor activity.

BIBR 1532 is a novel, specific telomerase inhibitor with IC50 = 93 nM.

A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 and caspase-7.

A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 and caspase-7.