Kinase Inhibitors

A cell-permeable and reversible benzimidazolo compound that acts as a potent and ATP-competitive inhibitor of Chk2 with an IC 50 of 15 nM and a K i of 37 nM. Displays ~ 1,000-fold greater selectivity over Cdk1/B and CK1 (IC 50 = 12 M and 17 M,

A cell-permeable naphthol derivative that acts as a highly potent and selective inhibitor of cAMP response element-binding protein (CREB)-mediated gene transcription (IC50 = 81 nM by CREB RLuc reporter assay with transfected HEK 293T cells). Also

Potentiates the activity of protein kinase C by inhibiting diacylglycerol metabolism. Inhibits diacylglycerol kinase (IC 50 = 2.

Application Diacylglycerol Kinase Inhibitor II has been used to determine tumor-induced inhibition with genetically modified cytotoxic T cells expressing chimeric antigen receptors (CAR). It has also been used to induce pAkt and PKR-like

Application Diacylglycerol Kinase Inhibitor II has been used to determine tumor-induced inhibition with genetically modified cytotoxic T cells expressing chimeric antigen receptors (CAR). It has also been used to induce pAkt and PKR-like

Inhibitor useful for elucidating roles of protein kinase C. Inhibits diacylglycerol (DAG) kinase in isolated platelet membranes (IC 50 = 300 nM) and in intact platelets (IC 50 = 120 nM).

A cell-permeable, orally bioavailable, blood-brain barrier permeant 2,6-diaminopyridine based compound that acts as a highly potent and selective inhibitor of dual leucine zipper kinase inhibitor (DLK K i = 500 pM). Exhibits an ideal balance of

A cell-permeable benzochromenone compound that acts as a potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK with an IC 50 of 0.23 &#181M.

A morpholino-benzophenone compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC 50 = 270 nM). Inhibits PI 3-K catalytic subunit p110-isozymes at higher concentrations (IC 50 = 32 &#181M, 3.

A cell-permeable 4,6-dianilinopyrimidine compound that acts as a potent, ATP-competitive, and highly selective inhibitor of EGFR and some EGFR mutants (IC 50 = 21 nM, 63 nM, and 4 nM for EGFRwt, EGFR L858R and EGFR L861Q , respectively) vs.

A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC 50 = 3 nM) and in culture (IC 50 = 0.15, 1.

A cell-permeable and reversible 13-amino acid peptide corresponding to the N-terminus of MAPK/ERK kinase (MEK or MAPKK) that is fused to the HIV-TAT membrane translocation peptide (MTP) sequence via a glycine linker. Acts as a specific inhibitor of