UK 5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC) that inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC50 = 50 nM). It decreases glucose flux to the TCA cycle and increases production of M6 citrate via glutaminolytic flux through malic enzymes without affecting...

EPI-001 is an androgen receptor antagonist with an IC50 value of approximately 6 µM for inhibition of transactivation of the androgen receptor N-terminal domain (NTD). It inhibits androgen-, FSK-, and IL-6-induced, as well as ligand-independent, prostate-specific antigen (PSA) reporter gene expression in LNCaP cells...

BQU57 is an inhibitor of the Ras-like GTPases RalA and RalB. It binds to RalB when RalB is bound to GDP with a Kd value of 7.7 µM, as determined by isothermal titration calorimetry (ITC). BQU57 (10 µM) decreases RalA and RalB activity in H2122 and H358 cells. It also inhibits colony formation of Ral-dependent H2122...

Bisdemethoxycurcumin (BDMC) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1alpha,25-dihydroxy vitamin D3 to stimulate amyloid-beta clearance by macrophages (optimal stimulation at 100 nM BDMC). More stable than curcumin in physiological media,...