Inhibitors

An enhanced in solution stable gallocyanine analog that directly and reversibly targets human LRP5/6 (low density lipoprotein-related protein 5/6), and disrupts its interaction with Dkk (Dickkopf) in a competitive manner. Shown to potently reverse

A 2-aminopyrimidine compound that counteracts the antagonizing effect of Dkk-1 (Dickkopf-1) against Wnt-3a/LRP5 interaction and prevents Dkk-1-mediated Kr2/LRP5/Dkk-1 complex formation and internalization. Shown to successfully rescue cellular

A cell-permeable bis -nitrobenzylidene-piperidinone that inhibits 19S deubiquitinase (DUB) activity (IC 50 = 2.1 &#181M against Ub-AMC hydrolysis) in a reversible manner by directly targeting UCH37/UCH-L5 and USP14, while exhibiting little or no

A cell-permeable dinitrobromobenzene compound that acts as a selective inhibitor of yeast Endoplasmic Reticulum Oxidase 1 (ERO1), but has somewhat weaker activity against mouse ERO1&#945 (IC 50 = 400 &#181M). Predicted to form thiol adducts and

A cell-permeable thiol reactive enone (EN) compound that selectively interacts with the active-site cysteine of reduced, active form of ERO1&#945 and inhibits its activity (IC 50 = 1.9 &#181M).

A cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 (IC 50 = 33 nM) over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in

A cell-permeable thiadiazolyl-butyl-pyridazinyl compound that selectively inhibits GLS1 (IC 50 = 23 nM &amp 28 nM, respectively, using murine kidney and brain homogenates), but not GLS2/LGA (up to 5 &#181M using murine liver homogenates),

A cell-permeable benzophenanthridinone compound that acts as an allosteric and reversible inhibitor of mitochondrial glutaminase activity and represses the growth and invasive activity in glutaminase upregulated fibroblasts and in tumor cells (IC

A weak inhibitor of the human and murine granzyme B. Also inhibits the apoptosis-related DNA fragmentation in lymphocytes by fragmentin 2, a rat lymphocyte granule protease homologous to granzyme B (ID 50 = 300 nM).

Biochem/physiol Actions Cell permeable: yes Product competes with ATP. Reversible: yes Packaging Packaged under inert gas Warning Toxicity: Carcinogenic / Teratogenic (D) Legal Information CALBIOCHEM is a registered trademark of Merck KGaA,

Biochem/physiol Actions Cell permeable: yes Product competes with ATP. Reversible: yes Packaging Packaged under inert gas Warning Toxicity: Carcinogenic / Teratogenic (D) Legal Information CALBIOCHEM is a registered trademark of Merck KGaA,

Biochem/physiol Actions Cell permeable: yes Product competes with ATP. Reversible: yes Packaging Packaged under inert gas Warning Toxicity: Carcinogenic / Teratogenic (D) Legal Information CALBIOCHEM is a registered trademark of Merck KGaA,