Biologically Active Small Molecules

A bile acid and FXR ligand (EC50 = 13-34 &muM) that is a key regulator of cholesterol homeostasis exhibits toxicity that is linked to increased glutathione and increased oxidative stress excess CDCA contributes to liver and intestinal cancers.

A natural product which acts as a small molecule inhibitor of HIF signaling, disrupting the binding of HIF-1&alpha and HIF-2&alpha to p300 at low nanomolar concentrations effectively attenuates the HIF pathway both in cells and in vivo, in mice.

A natural product which acts as a small molecule inhibitor of HIF signaling, disrupting the binding of HIF-1&alpha and HIF-2&alpha to p300 at low nanomolar concentrations effectively attenuates the HIF pathway both in cells and in vivo, in mice.

An HDAC inhibitor that increases histone H3 acetylation levels in LoVo and HT-29 colon cancer cells at concentrations as low as 4 &microM dose-dependently decreases the activation of several oncogenic signaling kinases and induces cell cycle

An HDAC inhibitor that increases histone H3 acetylation levels in LoVo and HT-29 colon cancer cells at concentrations as low as 4 &microM dose-dependently decreases the activation of several oncogenic signaling kinases and induces cell cycle

An HDAC inhibitor that increases histone H3 acetylation levels in LoVo and HT-29 colon cancer cells at concentrations as low as 4 &microM dose-dependently decreases the activation of several oncogenic signaling kinases and induces cell cycle

An HDAC inhibitor that increases histone H3 acetylation levels in LoVo and HT-29 colon cancer cells at concentrations as low as 4 &microM dose-dependently decreases the activation of several oncogenic signaling kinases and induces cell cycle

A selective, cell-permeable, quinolone-based inhibitor of Chk1 (IC₅₀ = 0.3 nM versus 0.

A selective, cell-permeable, quinolone-based inhibitor of Chk1 (IC₅₀ = 0.3 nM versus 0.

A selective, cell-permeable, quinolone-based inhibitor of Chk1 (IC₅₀ = 0.3 nM versus 0.

A selective, cell-permeable, quinolone-based inhibitor of Chk1 (IC₅₀ = 0.3 nM versus 0.

A reversible, cell-permeable inhibitor of GSK3&alpha and GSK3&beta (IC₅₀ = 0.65 and 0.