A selective inhibitor of NUAK1 and NUAK2 (IC<sub>50</sub>s = 20 and 100 nM, respectively) inhibits the phosphorylation of the NUAK1 substrate MYPT1 at Ser445 inhibits proliferation and migration of mouse embryonic fibroblasts and U2OS cells at 10
A selective inhibitor of NUAK1 and NUAK2 (IC<sub>50</sub>s = 20 and 100 nM, respectively) inhibits the phosphorylation of the NUAK1 substrate MYPT1 at Ser445 inhibits proliferation and migration of mouse embryonic fibroblasts and U2OS cells at 10
A full antagonist of RXR that demonstrates potent, nanomolar binding affinity does not affect the corepressor interaction capacity of the RAR&alpha subunit in the RAR-RXR heterodimer configuration.
A full antagonist of RXR that demonstrates potent, nanomolar binding affinity does not affect the corepressor interaction capacity of the RAR&alpha subunit in the RAR-RXR heterodimer configuration.
A non-steroidal androgen receptor antagonist (IC50 = 36 nM) reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.
A non-steroidal androgen receptor antagonist (IC50 = 36 nM) reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.
A selective inhibitor of diacylglycerol lipase (IC<sub>50</sub> = 4 µM) that demonstrates relatively weak inhibition of phospholipases A2 and C elevates the concentration of diacylglycerol, which leads to activation of PKC.
A selective inhibitor of diacylglycerol lipase (IC<sub>50</sub> = 4 µM) that demonstrates relatively weak inhibition of phospholipases A2 and C elevates the concentration of diacylglycerol, which leads to activation of PKC.
A potent, selective inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM) bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model decreases hepatic necrosis and apoptosis
A potent, selective inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM) bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model decreases hepatic necrosis and apoptosis
A selective inhibitor of NUAK1 and NUAK2 (IC<sub>50</sub>s = 20 and 100 nM, respectively) inhibits the phosphorylation of the NUAK1 substrate MYPT1 at Ser445 inhibits proliferation and migration of mouse embryonic fibroblasts and U2OS cells at 10
A selective inhibitor of NUAK1 and NUAK2 (IC<sub>50</sub>s = 20 and 100 nM, respectively) inhibits the phosphorylation of the NUAK1 substrate MYPT1 at Ser445 inhibits proliferation and migration of mouse embryonic fibroblasts and U2OS cells at 10
A selective inhibitor of the MAP kinases p38&alpha (IC<sub>50</sub> = 3.2 nM) and p38&beta (IC<sub>50</sub> = 122 nM) has no inhibitory effect against a panel of other kinases when tested in vitro at 50 &muM orally active, significantly
A selective inhibitor of the MAP kinases p38&alpha (IC<sub>50</sub> = 3.2 nM) and p38&beta (IC<sub>50</sub> = 122 nM) has no inhibitory effect against a panel of other kinases when tested in vitro at 50 &muM orally active, significantly
A non-steroidal androgen receptor antagonist (IC50 = 36 nM) reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.
A non-steroidal androgen receptor antagonist (IC50 = 36 nM) reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.
A selective inhibitor of diacylglycerol lipase (IC<sub>50</sub> = 4 µM) that demonstrates relatively weak inhibition of phospholipases A2 and C elevates the concentration of diacylglycerol, which leads to activation of PKC.
A selective inhibitor of diacylglycerol lipase (IC<sub>50</sub> = 4 µM) that demonstrates relatively weak inhibition of phospholipases A2 and C elevates the concentration of diacylglycerol, which leads to activation of PKC.