Autophagy Activators

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SML1822 Akebia saponin D ≥98% (HPLC) Akebia saponin D (ASD) is a bioactive triterpenoid saponin isolated from the rhizome of Dipsacus asper Wall that is used as an anti-osteoporosis drug. Akebia saponin D exhibits therapeutic effects in number of disease models including cancer, Alzheimer′s disease, cardiovascular disease, and bone fractures. Akebia saponin D protects against nonalcoholic fatty liver disease (NAFLD) liver damage in mice model of NAFLD. ASD decreases hepatic steatosis and heptocyte apoptosis through autophagy modulation. Akebia saponin D prevents oleic acid induced lipid droplets accumulation and increases autophagic flux BRL cells.
 
A8423 Amiodarone hydrochloride ≥98% Non-selective ion channel blocker with broad fungicidal activity. Amiodarone induces an immediate influx of Ca2+ in Saccharomyces cerevisiae, followed by mitochondrial fragmentation and cell death.
 
SRP5341 ATG13, GST tagged human recombinant, expressed in E. coli, ≥70% (SDS-PAGE), buffered aqueous glycerol solution   human ... ATG13(9776)
G2911 GF 109203X synthetic, ≥90% (HPLC) 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.
 
B6292 GF 109203X hydrochloride ≥95% Inhibitor of protein kinase C; potent inhibitor of GSK-3.
 
H6524 N-Hexanoyl-D-sphingosine ≥98% (TLC), synthetic Cell-permeable analog of ceramide; stimulates protein phosphatase 2A; activates MAP kinase; induces apoptosis in human leukemia HL-60 cells
 
SML1644 MRT68921 dihydrochloride ≥98% (HPLC) MRT68921 is a cell penetrant, potent and specific inhibitor of ULK1 and ULK2 kinases in vitro, which reduces ULK1 activity in cells and blocks autophagy induction. MRT68921 blocks mTOR dependent autophagy.
 
N3510 Niclosamide Niclosamide uncouples oxidative phosphorylation in the tapeworm and inhibits mitochondrial oxidative phosphorylation of parasitic helminths. It blocks tumor necrosis factor-induced IκBα phosphorylation, translocation of p65, and expression of NF-κΒ– regulated genes in AML cells.
 
SML0481 Qc1 ≥98% (HPLC) 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.
 
R0395 Rapamycin from Streptomyces hygroscopicus ≥95% (HPLC), powder 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.
human ... FKBP1A(2280)
R5648 Rottlerin 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.
human ... CDK2(1017)
S7448 STF-62247 ≥98% (HPLC), solid STF-62247 induces the formation of large vacuoles in the von Hippel-Lindau deficient renal carcinoma cells, a characteristic of autophagy.1
STF-62247 is a selective inducer of autophagy in VHL-deficient renal cell carcinoma cells.
 
T5648 Tamoxifen ≥99% 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.
human ... CYP1A2(1544), EBP(10682), ESR1(2099), ESR2(2100), ESRRA(2101)
rat ... Ar(24208), Esr1(24890)
PZ0020 Temsirolimus ≥98% (HPLC) 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.
 
SRP0252 ULK Active human recombinant, expressed in FreeStyle 293-F cells, ≥40% (SDS-PAGE) ULK1 (unc-51 like autophagy activating kinase 1) protein kinase plays a crucial role in the control of autophagy initiation. This protein is responsible for activating a cascade of signaling pathways which ultimately results in the formation of phagosomes. The phosphorylation of ULK1 by MTORC1 (mammalian target of rapamycin complex) leads to the negative regulation of autophagy. Activation of type I interferon (IFN) receptor (IFNR) results in the activation of ULK1 protein, which, in turn, results in the transcription of gene in a IFN-stimulated response elements (ISRE) and IFNγ activation site (GAS) elements-mediated manner. It is also required for the control of the expression of key IFN-stimulated genes (ISGs).
human ... ULK1(8408)
SML0176 Z36 ≥98% (HPLC) Z36 inhibits cell proliferation and induces death in HeLa cells. The cell death induced is via autophagy and autophagic flux.
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.