Autophagy Inhibitors

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189490 Autophagy Inhibitor, 3-MA - CAS 5142-23-4 - Calbiochem Autophagy Inhibitor, 3-MA, CAS 5142-23-4, is a cell-permeable autophagic sequestration blocker that protects cerebellar granule cells from apoptosis following serum/potassium deprivation., Autophagy Inhibitor, 3-MA, CAS 5142-23-4, is a cell-permeable autophagic sequestration blocker. Acts as an inhibitor of III PI3-Kinase.    
5.00554 mTOR Activator, MHY1485 - Calbiochem mTOR Activator, MHY1485, CAS Number: 326914-06-1, is a cell-permeable activator of mTOR that inhibits autophagy by suppressing the fusion between autophagosomes and lysosomes.    
5.34360 Autophagy Inhibitor VII - Calbiochem A cell-permeable, potent lysosome targeted autophagy inhibitor with reduced toxicity. OM: Supplied as HCl salt. After EA, will suitably recommend the changes.    
5.38355 ARN5187 - Calbiochem A cell-potent dual inhibitor of REV-ERBβ and autophagy. Relieves REV-ERB-mediated transcriptional repression and elicits stronger apoptotic induction in cancer cells.    
567569 Spautin-1 - Calbiochem A quinazolin compound that acts as a specific and potent inhibitor of autophagy and promotes Vps34 PI 3-kinase complex degradation by blocking the activity of USP 10 (IC₅₀ = 580 nM) and USP 13 (IC₅₀ = 690 nM) deubiquitinating enzymes    
A9165 N-Acetyl-L-cysteine cell culture tested, BioReagent Antioxidant and mucolytic agent. Increases cellular pools of free radical scavengers. Reported to prevent apoptosis in neuronal cells but induce apoptosis in smooth muscle cells. Inhibits HIV replication. May serve as a substrate for microsomal glutathione transferase.
 
A4159 L-Asparagine BioReagent, suitable for cell culture, suitable for insect cell culture    
B1793 Bafilomycin A1 from Streptomyces griseus ≥90% (HPLC) A specific inhibitor of vacuolar type H+-ATPase (V-ATPase) in animal cells, plant cells and microorganisms.
 
C3556   Catalase from human erythrocytes ≥90% (SDS-PAGE), buffered aqueous solution, ≥30,000 units/mg protein Catalase activates the decomposition of hydrogen peroxide, a reactive oxygen species, into water and oxygen. It functions as a natural antioxidant, protecting cells against oxidative damage to proteins, lipids and nucleic acids. Catalase has also been used to study the role reactive oxygen species play in gene expression and apoptosis.
Each subunit of the tetramer contains iron bound to a protoheme IX group. The enzyme also strongly binds NADP, which is in close proximity to the heme group. Catalase activity is constant over the pH range of 4.0-8.5. The pI is found to be 5.4. Optimum pH for catalytic activity is 7.0. The enzyme activity is inhibited by 3-amino-1-H-1,2,4 triazole, cyanide, azide, hydroxylamine, cyanogen bromide, 2-mercaptoethanol, dithiothreitol, dianisidine, and nitrate. Incubation of catalase with ascorbate or ascorbate/Cu2+ results in degradation of the catalase molecule.
human ... CAT(847)
C6628 Chloroquine diphosphate salt solid, ≥98% Standard anti-malarial drug. Substrate for MRP in multidrug resistant cell line and inhibits photoaffinity labeling of MRP by quinoline-based photoactive drug IAAQ (N-[4-[1-hydroxy-2-(dibutylamino)ethyl]quinolin-8-yl]-4-azidosalicylamide).
human ... ABCC1(4363)
SML0031 DBeQ ≥98% (HPLC) DBeQ is a potent and specific inhibitor of ATPase p97, an integral component of the ubiquitin-fusion degradation (UFD) pathway. DBeQ inhibits the degradation of ubiquitinated proteins, the endoplasmic reticulum-associated degradation pathway, and autophagosome maturation. The compound also potently inhibits cellular proliferation and induces caspase 3/7 activity and apoptosis.
 
E8640 E-64d protease inhibitor   human ... CAPN1(823)
SML0646   GMX1778 ≥98% (HPLC) GMX1778 (CHS-828) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) that exhibits a potent anticancer activity both in vitro and in vivo. GMX1778 exerts a cytotoxic effect by decreasing the cellular level of NAD+. GMX1778 increases intracellular ROS in cancer cells but does not induce ROS in normal cells.
 
L5793 Leupeptin BioUltra, microbial, ≥95% (HPLC) Inhibitor of serine and cysteine proteases. Inhibits plasmin, trypsin, papain, calpain, and cathepsin B. Does not inhibit pepsin, cathepsins A and D, thrombin, or α-chymotrypsin. Effective concentration 10-100 μM. There have been numerous studies using leupeptin to protect against hearing loss caused by acoustic overstimulation or the ototoxic antibiotic gentamicin. (Loss of cochlear hair cells is believed to be mediated by calpain.)
 
L9908 LY-294,002 hydrochloride solid, ≥98% (HPLC) Specific cell permeable phosphatidylinositol 3-kinase inhibitor.
 
M9281 3-Methyladenine autophagy inhibitor    
SML0810   MHY1485 ≥95% (HPLC) MHY1485 is mTOR activator that potently inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
 
P5318 Pepstatin A microbial, ≥90% (HPLC) Pepstatin A is an inhibitor of acid proteases (aspartyl peptidases). It forms a 1:1 complex with proteases such as pepsin, renin, cathepsin D, bovine chymosin, and protease B (Aspergillus niger). The inhibitor is highly selective and does not inhibit thiol proteases, neutral proteases, or serine proteases. Solubilized γ-secretase and retroviral protease are also inhibited by Pepstatin A. It has been used to characterize proteases from several sources.
 
SML1540 SBI-0206965 ≥98% (HPLC) SBI-0206965 is a potent and selective inhibitor of the serine/threonine autophagy-initiating kinases ULK1 and ULK2 with selectivity for ULK1. SBI-0206965 has an IC50 value of 108 nM for ULK1, compared to 711nM for ULK2. Tumor cells require autophagy to remove misfolded proteins or damaged cellular organelles. SBI-0206965 was shown to suppress autophagy induced by mTOR inhibition. mTOR signaling is often hyperactive in many tumors and can drive proliferation, so mTOR inhibitors are being investigated as anticancer agents. However, mTOR inhibition also results in activation of the ULK1-dependent autophagy survival response, and most results with mTOR inhibitors have been at best cytostatic. SBI-0206965 synergizes with mTOR inhibition to induce apoptosis and cell death.
 
SML0440 Spautin-1 ≥98% (HPLC) Spautin-1 inhibits the activity of two ubiquitin-specific peptidases, USP10 and USP13, causing an increase in proteasomal degradation of class III PI3 kinase complexes, which have been shown to regulate autophagy.
 
T9033 Thapsigargin ≥98% (HPLC), solid film Potent, cell-permeable, IP3-independent intracellular calcium releaser. Blocks the transient increase in intracellular Ca2+ induced by angiostatin and endostatin. Induces apoptosis by disrupting intracellular free Ca2+ levels; incorporated into chemotherapeutic prodrug formulations.
 
W1628 Wortmannin from Penicillium funiculosum, ≥98% (HPLC and TLC) Wortmannin is a potent and specific phosphatidylinositol 3-kinase (PI3-K) inhibitor with an IC50 of 2-4 nM. Inhibition of PI3-K/Akt signal transduction cascade enhances the apoptotic effects of radiation or serum withdrawal and blocks the antiapoptotic effect of cytokines. Inhibition of PI3-K by wortmannin also blocks many of the short-term metabolic effects induced by insulin receptor activation.
human ... PIK3CD(5293), PIK3CG(5294), PIK3R1(5295)