Biologically Active Small Molecules

An inhibitor of PDKs, resulting in an increase in PDH activity (EC₅₀ = 5.2 nM for PDK2) less potently inhibits PDK1 and PDK3 (IC₅₀s = 87 and 600 nM, respectively).

An inhibitor of PDKs, resulting in an increase in PDH activity (EC₅₀ = 5.2 nM for PDK2) less potently inhibits PDK1 and PDK3 (IC₅₀s = 87 and 600 nM, respectively).

An inhibitor of PDKs, resulting in an increase in PDH activity (EC₅₀ = 5.2 nM for PDK2) less potently inhibits PDK1 and PDK3 (IC₅₀s = 87 and 600 nM, respectively).

An inhibitor of PDKs, resulting in an increase in PDH activity (EC₅₀ = 5.2 nM for PDK2) less potently inhibits PDK1 and PDK3 (IC₅₀s = 87 and 600 nM, respectively).

Selectively inhibits checkpoint kinases Chk1 and Chk2 (IC50s = 5 nM) abrogates DNA damage-induced S and G2 checkpoints (EC50 = 10 nM) and potentiates the efficacy of gemcitabine and topotecan by modulating downstream checkpoint pathway proteins.

Selectively inhibits checkpoint kinases Chk1 and Chk2 (IC50s = 5 nM) abrogates DNA damage-induced S and G2 checkpoints (EC50 = 10 nM) and potentiates the efficacy of gemcitabine and topotecan by modulating downstream checkpoint pathway proteins.

Selectively inhibits checkpoint kinases Chk1 and Chk2 (IC50s = 5 nM) abrogates DNA damage-induced S and G2 checkpoints (EC50 = 10 nM) and potentiates the efficacy of gemcitabine and topotecan by modulating downstream checkpoint pathway proteins.

Selectively inhibits checkpoint kinases Chk1 and Chk2 (IC50s = 5 nM) abrogates DNA damage-induced S and G2 checkpoints (EC50 = 10 nM) and potentiates the efficacy of gemcitabine and topotecan by modulating downstream checkpoint pathway proteins.

A potent, selective ATP-competitive inhibitor of mTOR (IC₅₀ = 0.8 nM) inhibits proliferation of A549 (IC₅₀ = 53 nM) and H838 cells (IC₅₀ = 20 nM) as well as several human tumor xenografts (&gt65% at 20 mg/kg).

A potent, selective ATP-competitive inhibitor of mTOR (IC₅₀ = 0.8 nM) inhibits proliferation of A549 (IC₅₀ = 53 nM) and H838 cells (IC₅₀ = 20 nM) as well as several human tumor xenografts (&gt65% at 20 mg/kg).

A potent, selective ATP-competitive inhibitor of mTOR (IC₅₀ = 0.8 nM) inhibits proliferation of A549 (IC₅₀ = 53 nM) and H838 cells (IC₅₀ = 20 nM) as well as several human tumor xenografts (&gt65% at 20 mg/kg).

A potent, selective ATP-competitive inhibitor of mTOR (IC₅₀ = 0.8 nM) inhibits proliferation of A549 (IC₅₀ = 53 nM) and H838 cells (IC₅₀ = 20 nM) as well as several human tumor xenografts (&gt65% at 20 mg/kg).