Kinase Inhibitors

A cell-permeable symmetrical disulfide allosteric inhibitor that selectively targets the autoregulatory domain of group I, but not group II, PAKs (p21-activated kinases) and prevents the activation of PAK1/2/3 (% inhibition= 95, 70, and 60,

A cell-permeable methylsulfanylimidazole compound that acts as a potent, selective, reversible, and ATP-competitive p38 MAP kinase inhibitor (IC 50 = 0.38 &#181M for p38&#945).

A cell-permeable symmetrical sulfone compound that acts as a potent and ATP-competitive inhibitor of p38&#945/&#946 MAPK (IC 50 = 130 and 550 nM, respectively), while exihibiting much reduced activity (&#880423% inhibition at 1 &#181M) against

A cell-permeable indole compound that acts as a potent, ATP-competitive, and isozyme-selective p38&#945 MAP kinase inhibitor (IC 50 = 3.2 nM).

A cell-permeable, water soluble and specific p53-Snail binding inhibitor that activates p53 in a K-Ras-dependent manner and displays anti-proliferating effect toward K-Ras-MEF (K-Ras-transformed mouse embryonic fibroblast) cells with 20% viability

A cell-permeable indenopyrazole compound that displays potent antiproliferative properties in several human tumor cell lines (IC 50 &lt33 nM). Shown to act as an ATP-competitive and reversible inhibitor of PDGFR (IC 50 = 4.

A cell-permeable quinolinyl-thiourea compound that acts a potent, ATP-competitive, and reversible inhibitor of PDGFR (IC 50 = 4 and 7.6 nM in ligand-induced cellular PDGFR phosphorylation and in in vitro kinase activity, respectively).

A cell-permeable pyrrolopyrimidinamine compound that acts as a potent, ATP-competitive EIF2AK3/PERK inhibitor (IC 50 = 0.9 nM [ATP] = 10 &#181M), displaying &#8805511-fold selectivity over HRI/EIF2AK1, BRK, PKR/EIF2AK2, and MEKK2 (IC 50 = 460,

A cell-permeable isoflavone compound that acts as a potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3 IC 50 = 670 nM K i = 240 nM). Directly docks into the Fru-6-P binding pocket of PFKFB3 and down-regulates Fru-2,6-BP

An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC 50 = 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively K i = 5 nM for PIM-1) with excellent selectivity

A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive inhibitor against Pim-1/2 kinases (IC 50 = 150 nM and 20 nM against Pim-1 and Pim-2, respectively) as well as DYRK1&#945 (68% inhibition of DYRK1&#945 and Pim-2 at

A cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (K i = 0.3 &#181M), and highly isoform-selective PIM inhibitor (IC 50 = 2.