2. Signaling Pathways
  3. Autophagy
  4. Autophagy

Autophagy

Autophagy

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Autophagy is a conserved cellular degradation and recycling process in the lysosome. In mammalian cells, there are three primary types of autophagy: microautophagy, macroautophagy, and chaperone-mediated autophagy (CMA). Microphagy captures cargoes by means of invaginations or protrusions of the lysosomal membrane directly, CMA uses chaperones to identify cargo proteins and then unfolds and transfers them into the lysosomal, while macroautophagy sequesters cargo by autophagosomes-de novo synthesized of double-membrane vesicles-and subsequently transport it to the lysosome.

Macroautophagy is the best studied and it occurs at a low level constitutively and can also be further induced under stress conditions, such as nutrient or energy starvation with a salient feature of autophagy protein degradation. Stress-induced macrophagy plays an important role in protein catabolism with another key protein degradation pathway, the ubiquitin–proteasome system (UPS).

As the study progressed, autophagy gains its importance under basal, nutrient-rich conditions, and is now recognized as a critical housekeeping pathway in catabolism of diverse cellular constituents, such as protein aggregates (aggrephagy), lipid droplets (lipophagy), iron complex (Ferritinophagy) and carbohydrate. Except for macromolecules, autophagy can also target several organelles and structures, such as mitochondria (mitophagy), peroxisome (pexophagy), endoplasmic reticulum (reticulophagy or ER-phagy), ribosome (ribophagy), spermatozoon-inherited organelles following fertilization (allophagy), secretory granules within pancreatic cells (zymophagy) and intracellular pathogens (xenophagy).

Autophagy and its dysfunction are associated with a variety of human pathologies, including ageing, cancer, neurodegenerative disease, heart disease and metabolic diseases, such as diabetes. Plenty of drugs and natural products are involved in autophagy modulation through multiple signaling pathways. Small molecules that can regulate autophagy seem to have great potential to intervene such diseases in animal models or clinical courses.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13271A
    Tubastatin A
    		Inducer 98.37%
    Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
    Tubastatin A
  • HY-10256A
    Adezmapimod hydrochloride
    		Inducer 99.71%
    Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator.
    Adezmapimod hydrochloride
  • HY-N0155
    Nobiletin
    		Inducer 99.79%
    Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.
    Nobiletin
  • HY-44134
    Dimethyl 2-oxoglutarate
    		Inhibitor
    Dimethyl 2-oxoglutarate (Dimethyl α-ketoglutarate), a cell permeable 2-oxoglutarate derivative, is a tricarboxylic acid cycle metabolite with antioxidant properties. Dimethyl 2-oxoglutarate serves as a crucial intermediate in the Krebs cycle and an essential nitrogen carrier in metabolic pathways during biological processes. Dimethyl 2-oxoglutarate inhibits autophagy in an IDH1-, IDH2- and ACLY-dependent fashion in cultured human cells. Dimethyl 2-oxoglutarate efficiently prevents autophagy induced by starvation in mice.
    Dimethyl 2-oxoglutarate
  • HY-10215
    Luminespib
    		Inducer 99.81%
    Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
    Luminespib
  • HY-15025
    Sildenafil
    		Inducer 99.90%
    Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
    Sildenafil
  • HY-15097
    Myricetin
    		Inducer 98.42%
    Myricetin is a common plant-derived flavonoid with a wide range of activities including strong anti-oxidant, anticancer, antidiabetic and anti-inflammatory activities.
    Myricetin
  • HY-12990
    Spautin-1
    		Inhibitor 99.54%
    Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.
    Spautin-1
  • HY-N1362
    Salvianolic acid B
    		Inducer 99.92%
    Salvianolic acid B is an active ingredient of Salvia miltiorrhiza, which has been widely applied in China for the management of various microcirculation-related disorders, such as cardiovascular disease, cerebrovascular disease, and diabetic vascular complication.
    Salvianolic acid B
  • HY-13002
    Torin 2
    		Inducer 99.65%
    Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
    Torin 2
  • HY-50946
    Imatinib Mesylate
    		Inducer 99.98%
    Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
    Imatinib Mesylate
  • HY-13074
    VO-Ohpic trihydrate
    		≥98.0%
    VO-Ohpic trihydrate is a highly potent inhibitor of PTEN with an IC50 of 46±10 nM.
    VO-Ohpic trihydrate
  • HY-17376
    Ezetimibe
    		Inducer 99.72%
    Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
    Ezetimibe
  • HY-16989
    SR9009
    		Inhibitor 99.46%
    SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
    SR9009
  • HY-100437
    HA15
    		99.98%
    HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
    HA15
  • HY-10182A
    Laduviglusib monohydrochloride
    		Inducer 99.93%
    Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy.
    Laduviglusib monohydrochloride
  • HY-119240
    CCT020312
    		99.05%
    CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
    CCT020312
  • HY-B0246
    Carbamazepine
    		Inducer 99.95%
    Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC50 of 131 μM. Carbamazepine blocks voltage gated Na+, Ca2+, and K+ channels, and is also a HDAC inhibitor (IC50: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain.
    Carbamazepine
  • HY-19824
    3PO
    		Inhibitor 99.85%
    3PO is an inhibitor of PFKFB3. 3PO attenuates the proliferation of several cancer cell lines with IC50s of 1.4-24 μmol/L. 3PO suppresses glucose uptake and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+ and NADH. 3PO can be used for the research of cancer.
    3PO
  • HY-N0191
    Andrographolide
    		Inducer 99.74%
    Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
    Andrographolide
Cat. No. Product Name / Synonyms Application Reactivity
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