Activators & Inhibitors

Ruxolitinib, also known as INCB18424, is a potent and selective Janus kinase JAK1 and JAK2 inhibitor, with IC50s of 5.9 nM and 5.7 nM, respectively. It inhibited IL-6 and IL-23 effects at concentrations less than 50 nM. Ruxolitinib was effective in the rat adjuvant arthritis model and multiple murine models of arthritis.

Ruxolitinib, also known as INCB18424, is a potent and selective Janus kinase JAK1 and JAK2 inhibitor, with IC50s of 5.9 nM and 5.7 nM, respectively. It inhibited IL-6 and IL-23 effects at concentrations less than 50 nM. Ruxolitinib was effective in the rat adjuvant arthritis model and multiple murine models of arthritis.

NLG919 is an orally available potent inhibitor of the indoleamine-2,3- dioxygenase (IDO1) pathway, a crucial pathway involved in allergic inflammation that mediates immunosuppressive effects through metabolization of tryptophan to kynurenine. NLG919 affects differentiation and proliferation of T cells by inducing downstream signaling via GCN2, mTOR and AHR, with values of Ki = 7 nM and EC50 = 75 nM. NLG919 is being investigated for the treatment of immunosuppression associated with cancer.

NLG919 is an orally available potent inhibitor of the indoleamine-2,3- dioxygenase (IDO) pathway, a crucial pathway involved in allergic inflammation that mediates immunosuppressive effects through metabolization of tryptophan to kynurenine. NLG919 affects differentiation and proliferation of T cells by inducing downstream signaling via GCN2, mTOR and AHR, with values of Ki = 7 nM and EC50 = 75 nM. NLG919 is being investigated for the treatment of immunosuppression associated with cancer.

INCB024360 analog is an orally available hydroxyamidine and inhibitor of indoleamine 2,3- dioxygenase (IDO1), with an IC_50?? of 10 nM. It shows little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). INCB024360 analog displays potential immunomodulating and antineoplastic activities.

INCB024360 analog is an orally available hydroxyamidine and inhibitor of indoleamine 2,3- dioxygenase (IDO1), with an IC??₅₀ of 10 nM. It shows little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). INCB024360 analog 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.

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.