Biologically Active Small Molecules

A selective inhibitor of MCT1 (Ki = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport increases intratumor lactate levels and decreases tumor growth in mice bearing SCLC xenografts.

A selective inhibitor of the fibroblast growth factor receptor tyrosine kinase (IC₅₀s = 0.2, 2.

A selective inhibitor of the fibroblast growth factor receptor tyrosine kinase (IC₅₀s = 0.2, 2.

A selective inhibitor of the fibroblast growth factor receptor tyrosine kinase (IC₅₀s = 0.2, 2.

A pan-Akt inhibitor (Akt1, 2, and 3 IC₅₀s = 3, 7, and 7 nM, respectively) that also inhibits P70S6K and PKA (IC₅₀s = 6 and 7 nM, respectively) and shows &gt75% inhibition at 1 &muM against ROCK-II, MKK1, MSK1, MSK2,

A pan-Akt inhibitor (Akt1, 2, and 3 IC₅₀s = 3, 7, and 7 nM, respectively) that also inhibits P70S6K and PKA (IC₅₀s = 6 and 7 nM, respectively) and shows &gt75% inhibition at 1 &muM against ROCK-II, MKK1, MSK1, MSK2,

A pan-Akt inhibitor (Akt1, 2, and 3 IC₅₀s = 3, 7, and 7 nM, respectively) that also inhibits P70S6K and PKA (IC₅₀s = 6 and 7 nM, respectively) and shows &gt75% inhibition at 1 &muM against ROCK-II, MKK1, MSK1, MSK2,

A pan-Akt inhibitor (Akt1, 2, and 3 IC₅₀s = 3, 7, and 7 nM, respectively) that also inhibits P70S6K and PKA (IC₅₀s = 6 and 7 nM, respectively) and shows &gt75% inhibition at 1 &muM against ROCK-II, MKK1, MSK1, MSK2,

A potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14-99 and 530 nM, respectively) weakly inhibits EGFR (IC50 = 7.0 &microM) and has no effect on a large panel of other kinases suppresses growth and induces apoptosis and

A potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14-99 and 530 nM, respectively) weakly inhibits EGFR (IC50 = 7.0 &microM) and has no effect on a large panel of other kinases suppresses growth and induces apoptosis and

A potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14-99 and 530 nM, respectively) weakly inhibits EGFR (IC50 = 7.0 &microM) and has no effect on a large panel of other kinases suppresses growth and induces apoptosis and

A potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14-99 and 530 nM, respectively) weakly inhibits EGFR (IC50 = 7.0 &microM) and has no effect on a large panel of other kinases suppresses growth and induces apoptosis and