Inhibitors

A cell-permeable dihydropyrazinyl-thioacetamide that acts as an ATP-competitive MARK inhibitor (IC 50 = 3.6 &#181M [ATP] = 100 &#181M) with much reduced or little activity against GSK-3&#946, SAD-kinase B/BRSK-1, MARKK/TAO-1, Cdc2/cycB, and

A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic &#945-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC 50 = 11 nM for [ 14 C]-lactate uptake in rat brain endothelial cell line

A cell-permeable pyrole pyrimidine-based compound that acts as an inhibitor of monocarboxylate transporter 1 (MCT1, SLC16A1) and blocks the proliferation of Raji Burkitt lymphoma (Raji BL) cells expressing MCT1 (EC 50 = 5 nM). Also shown to inhibit

A cell-permeable tetrahydro-&#946-carbolinylbarbiturate compound that selectively inhibits the E3 ligase activity of Mdm2-MdmX hetero-complex over that of Mdm2-Mdm2 homo-complex (70.6% vs.

A cell-permeable quinazolinone compound that inhibits yeast (Dnm1) and mammalian (Drp1) division DRPs (dynamin-related GTPases) and effectively induces mitochondrial fusion into net-like structures (IC 50 = 10 and 50 M in yeast and COS cultures,

A cell-permeable furanylcarboxamide compound that acts as a potent, reversible and non-ATP-competitive inhibitor of MK-2/MAPKAP-K2 activity (IC 50 = 110 nM EC 50 = 350 nM for pHSP27 in IL-1&#946-stimulated SW1353 cells) with excellent selectivity

A cell-permeable, potent inhibitor of MMP-2 that acts in a dose-dependent manner (K i = 1.7 &#181M).

A cell-permeable biphenylsulfonylvaline compound that acts as a potent inhibitor against MMP-2, -3, and -13 (IC 50 = 47, 12, and 8 nM, respectively) and a weaker inhibitor against AMP deaminase (20% inhibition at 0.1 &#181M), MMP-1, -7, -9, and

A potent inhibitor of MMP-2 (IC 50 = 310 nM) and MMP-9 (IC 50 = 240 nM). Orally active in animal models of tumor growth and metastasis.

A potent inhibitor of MMP-2 (IC 50 = 17 nM) and MMP-9 (IC 50 = 30 nM). Also shown to potently induce and rapidly activate HIF.

This compound is a cell-permeable, selective, and reversible thiopyrimidone MMP-9 allosteric inhibitor that binds specifically to the non-catalytic site of MMP-9 at the PEX domain with a K d = 2.1 &#181M and thereby disrupts MMP-9 homodimerization

A cell-permeable thieno[2,3-d]pyrimidinedione compound that acts as a highly potent inhibitor of monocarboxylate transporter 1 (MCT1 K i = 2.3 nM for lactate uptake in rat erythrocytes).