A potent and selective competitive inhibitor of protein kinase C (PKC) and of glycogen synthase kinase-3 (GSK-3). In certain cells, inhibition of PKC leads to an increase in autophagy. For PKC inhibition, typically used at a concentration of 0.1-10 μM. A potent and selective competitive inhibitor of protein kinase C (PKC) and of glycogen synthase kinase-3 (GSK-3). Inhibits parathyroid hormone-induced Ca2+ resorption from isolated bone tissue, Staurosporine, another protein kinase inhibitor, actually enhanced Ca2+ resorption elicited by a number of agents, but GF109203X counteracted that enhancement.1
Niclosamide is used to study the Wnt/Frizzled-1 signaling pathway. It inhibits mitochondrial oxidative phosphorylation of parasitic helminths. Niclosamide uncouples oxidative phosphorylation in the tapeworm. It inhibits mitochondrial oxidative phosphorylation of parasitic helminths. It inhibits the NF-κB pathway in acute myelogenous leukemia (AML) cells. Niclosamide inhibits the transcription and DNA binding of NF-κB. It blocks tumor necrosis factor-induced IκBα phosphorylation, translocation of p65, and expression of NF-κB– regulated genes in AML cells. It increases ROS levels to induce apoptosis in AML cells1.
Qc1 is a reversible inhibitor of threonine dehydroxygenase (TDH). The IC50 value for inhibition of TDH by Qc1 is 500 nM, with no detectable inhibition of other dehydroxygenase enzymes at concentrations up to 10 mM. Qc1 induces arrest and autophagy of mouse ES cells with an EC50 of 3 mM.
A macrocyclic triene antibiotic that binds to and inhibits the molecular target of rapamycin (mTOR). It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). Rapamycin is a potent immunosuppressant and has anticancer activity.
Recently, Rottlerin (mallotoxin) has been shown to be a potent activator of the large conductance voltage and Ca2 activated K+ channel and to potently leftward shift the conductance-voltage relationship of the channel. Mallatoxin tested on hERG channels increased both step and tail hERG current by leftward shifting the voltage dependence of hERG activation and slowing channel deactivation. These actions distinguish Mallatoxin as a novel naturally occurring hERG channel activator.
Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.
Temsirolimus is a specific inhibitor of mammalian target of rapamycin (mTOR) mTOR Complex 1 (mTORC1). Temsirolimus is an antiproliferative and antiangiogenic, the first-in-class mTOR inhibitor approved for the treatment of patients with advanced poor prognosis renal cell carcinoma.
Z36 is a Bcl-XL inhibitor that induces autophagic cell death independent of apoptosis which distinguishes it from other Bcl-XL and Bcl-2 inhibitors that induce cancer cell death mainly through apoptosis. Z36 binds to the BH3 binding groove of BCL-XL where it is thought to induce autophagy through blocking the interaction between Bcl-XL/Bcl2 and Beclin 1.