Biologically Active Small Molecules

A secondary metabolite produced by some species of lichen that binds FAS-II enzymes to produce antibacterial and antiplasmodial effects inhibits PfFabZ and PfFabI (IC₅₀ = 10.7 and 36.

A hydroxyethyl ether rapamycin derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM orally available with superior pharmacokinetics and pharmacodynamics over rapamycin.

A hydroxyethyl ether rapamycin derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM orally available with superior pharmacokinetics and pharmacodynamics over rapamycin.

A hydroxyethyl ether rapamycin derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM orally available with superior pharmacokinetics and pharmacodynamics over rapamycin.

EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-&beta receptor type 1 IC₅₀ = 12.9 nM).

EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-&beta receptor type 1 IC₅₀ = 12.9 nM).

EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-&beta receptor type 1 IC₅₀ = 12.9 nM).

A cell-permeable, selective inhibitor of SIRT1 (IC50 = 98 nM) inhibits other SIRTs only at much higher concentrations and has no effect on other HDACs.

A cell-permeable, selective inhibitor of SIRT1 (IC50 = 98 nM) inhibits other SIRTs only at much higher concentrations and has no effect on other HDACs.

A cell-permeable, selective inhibitor of SIRT1 (IC50 = 98 nM) inhibits other SIRTs only at much higher concentrations and has no effect on other HDACs.

A third generation, irreversible steroidal aromatase inhibitor (Ki = 10.2 nM Kinact = 26 nM) that induces aromatase degradation, which leads to a decrease in estrogen levels in plasma.

A third generation, irreversible steroidal aromatase inhibitor (Ki = 10.2 nM Kinact = 26 nM) that induces aromatase degradation, which leads to a decrease in estrogen levels in plasma.