Chemicals & Small Molecules

Epacadostat (INCB024360) is an orally available hydroxyamidine and inhibitor of indoleamine 2,3- dioxygenase (IDO1), with an IC₅₀?? of 10 nM. It shows little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat displays potential immunomodulating and antineoplastic activities.

Epacadostat (INCB024360) is an orally available hydroxyamidine and inhibitor of indoleamine 2,3- dioxygenase (IDO1), with an IC₅₀?? of 10 nM. It shows little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat displays potential immunomodulating and antineoplastic activities.

PI-103 is a multi-targeted inhibitor of PI3K for p110?, p110?, p110 ?, and p110? with reported IC50 values of 2 nM, 3 nM, 3 nM, and 15 nM respectively. PI-103 is less potent towards mTOR/DNA-PK with reported IC50 values of 30 nM and 23 nM respectively.

PI-103 is a multi-targeted inhibitor of PI3K for p110?, p110?, p110 ?, and p110? with reported IC50 values of 2 nM, 3 nM, 3 nM, and 15 nM respectively. PI-103 is less potent towards mTOR/DNA-PK with reported IC50 values of 30 nM and 23 nM respectively.

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.

AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.