Biologically Active Small Molecules

An orally bioavailable inhibitor of PARP1 and PARP2 (Kis = 5.2 and 2.9 nM, respectively) enhances apoptosis and autophagy in response to treatments that cause DNA breaks, including radiation and DNA alkylation.

An orally bioavailable inhibitor of PARP1 and PARP2 (Kis = 5.2 and 2.9 nM, respectively) enhances apoptosis and autophagy in response to treatments that cause DNA breaks, including radiation and DNA alkylation.

An orally bioavailable inhibitor of PARP1 and PARP2 (Kis = 5.2 and 2.9 nM, respectively) enhances apoptosis and autophagy in response to treatments that cause DNA breaks, including radiation and DNA alkylation.

A high affinity agonist of TSPO (Ki = 0.297 nM in rat whole brain) that exhibits IC₅₀ values of 2.

A high affinity agonist of TSPO (Ki = 0.297 nM in rat whole brain) that exhibits IC₅₀ values of 2.

A high affinity agonist of TSPO (Ki = 0.297 nM in rat whole brain) that exhibits IC₅₀ values of 2.

A selective PAR2 agonist that stimulates cell proliferation, phosphatidylinositol hydrolysis, and calcium mobilization in in vitro functional assays (pEC₅₀s = 6.7, 5.9, and 6.6, respectively) elicits pronociceptive activity in vivo.

A selective PAR2 agonist that stimulates cell proliferation, phosphatidylinositol hydrolysis, and calcium mobilization in in vitro functional assays (pEC₅₀s = 6.7, 5.9, and 6.6, respectively) elicits pronociceptive activity in vivo.

A selective PAR2 agonist that stimulates cell proliferation, phosphatidylinositol hydrolysis, and calcium mobilization in in vitro functional assays (pEC₅₀s = 6.7, 5.9, and 6.6, respectively) elicits pronociceptive activity in vivo.

A selective PAR2 agonist that stimulates cell proliferation, phosphatidylinositol hydrolysis, and calcium mobilization in in vitro functional assays (pEC₅₀s = 6.7, 5.9, and 6.6, respectively) elicits pronociceptive activity in vivo.

An acetylated synthetic peptide from human calpastatin that strongly inhibits both calpains I and II but not papain or trypsin.

An acetylated synthetic peptide from human calpastatin that strongly inhibits both calpains I and II but not papain or trypsin.