Biologically Active Small Molecules

An orally available, reversible inhibitor of Akt (Ki = 11 nM for Akt1) also inhibits PKA and Cdk2 with IC₅₀ values of 16 and 46 nM, respectively reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor

A potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC₅₀ = 3.2 and 26 &microM, respectively).

A potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC₅₀ = 3.2 and 26 &microM, respectively).

A potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC₅₀ = 3.2 and 26 &microM, respectively).

A small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.

A small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.

A small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.

A-77-01 is a potent inhibitor of the TGF-&beta1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways.

A-77-01 is a potent inhibitor of the TGF-&beta1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways.

A-77-01 is a potent inhibitor of the TGF-&beta1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways.

A-77-01 is a potent inhibitor of the TGF-&beta1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways.

Reversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC₅₀s = 0.09, 3.