Calcium Signaling Agents

A potent and irreversible inhibitor of caspase-9 (ICE-LAP6, Mch6). Reported to reduce myocardial infarct size during reperfusion (~70 nM).

An internally quenched, highly cathepsin K-selective, fluorogenic peptide substrate that is efficiently cleaved by CatK ( k cat /K m = 0.426 &#181M -1 S -1 ), but not by Cathepsins B/L/S/F/H/V.

An epoxysuccinyl peptide highly selective for rat liver cathepsin L (IC 50 = 1.9 nM), while exhibiting little to no effect on rat liver cathepsin B at concentrations higher than 1000-5000 nM, in vitro .

A cell-permeable pyrazolo-pyrimidinone compound that acts as a potent, selective, and ATP-competitive inhibitor of Cdks (IC 50 = 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively).

A cell-permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC 50 = 20 nM, 35 nM and 92 nM in HCT-116, HeLa, and A375 cells, respectively). Acts as a highly potent, reversible,

A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC 50 = 0.5 &#181M for Cdk2/A and Cdk2/E 4.

A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC 50 = 0.5 &#181M for Cdk2/A and Cdk2/E 4.

A cell-permeable aminopyrimidinyl compound that acts as a potent and ATP-competitive inhibitor of Cdk2/E and Cdk9/T1 (K i = 2 nM and 4 nM, respectively). It also inhibits GSK-3&#946, Cdk4/D 1 , Cdk7/H, Cdk1/B, and Abl at higher concentrations (K i

A cell-permeable azo-pyrazole compound that acts as a potent, ATP-competitive, and Cdk9-selective inhibitor (IC 50 = 350 nM, using Cdk9/T1). It inhibits Cdk1/B, Cdk2/E, Cdk2/A, Cdk4/D1, Cdk7/H, and p70S6K only at much higher concentrations (IC 50 =

A cell-permeable, non-Hemicholinium-3 derivative and choline-competitive choline kinase-&#945 inhibitor. It is demonstrated to inhibit endogenous choline kinase activity, dose-dependently, between 1-10 &#181M, and dose-dependently decrease

A cell-permeable indazolylimidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC 50 = 2 nM) with moderate selectivity over TrkA, GSK-3&#946, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100

A cell-permeable ureidocarboxamido thiophene compound that acts as a potent, reversible, and ATP-competitive inhibitor of IKK-2 (IC 50 = 18 nM) with selectivity over IKK-1, JNK and p38 MAPK. Inhibits TNF-&#945 production in human monocytes (IC 50