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-110032
    Lamotrigine isethionate
    		Inhibitor
    Lamotrigine (BW430C) isethionate is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine isethionate selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine isethionate can be used for the research of epilepsy, focal seizure, et al.
    Lamotrigine isethionate
  • HY-13271B
    Tubastatin A TFA
    		Inducer
    Tubastatin A (TSA) TFA is a potent and selective?HDAC6?inhibitor with?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 TFA also inhibits HDAC10 and metallo-β-lactamase domain-containing protein?2 (MBLAC2).
    Tubastatin A TFA
  • HY-19805A
    STO-609 acetate
    STO-609 acetate is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 acetate inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
    STO-609 acetate
  • HY-117985
    Evogliptin
    		Inducer
    Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.
    Evogliptin
  • HY-10058
    AT9283 lactic acid
    		Inducer
    AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo.
    AT9283 lactic acid
  • HY-14654A
    Aspirin lithium
    		Inducer
    Aspirin (Acetylsalicylic Acid) lithium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
    Aspirin lithium
  • HY-110067
    VO-OHPic
    		Inhibitor
    VO-OHPic is a reversible, noncompetitive and selective PTEN inhibitor with an IC50 of 46 nM. VO-OHPic attenuates apoptosis, adverse cardiac remodeling, and pro-inflammatory M1 macrophages in doxorubicin-induced cardiomyopathy. VO-OHPic inhibits autophagy.
    VO-OHPic
  • HY-B1232A
    Metyrapone Tartrate
    		Activator
    Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression.
    Metyrapone Tartrate
  • HY-10341C
    Fasudil dihydrochloride
    		Inducer
    Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator.
    Fasudil dihydrochloride
  • HY-173119
    SKLB-D18
    		Agonist
    SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50s of 38.69, 40.12 and 59.72 nM, respectively. SKLB-D18 is also an autophagy agonist, plays a role in mTOR/p70S6K and NCOA4-mediated ferroptosis, which may mitigate multidrug resistance. SKLB-D18 exhibits significantly superior efficacy in vitro and in vivo against triple-negative breast cancer (TNBC).
    SKLB-D18
  • HY-12176B
    Aliskiren fumarate
    		Inducer
    Aliskiren fumarate is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren fumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
    Aliskiren fumarate
  • HY-50866B
    NVP-AEW541 dihydrochloride
    		Inducer
    NVP-AEW541 dihydrochloride (AEW541 dihydrochloride) is an orally active inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with an IC50 value of 0.15 μM. NVP-AEW541 dihydrochloride also inhibits InsR, IC50 with a value of 0.14 μM. NVP-AEW541 dihydrochloride has antitumor activity.
    NVP-AEW541 dihydrochloride
  • HY-B0495A
    Lamotrigine hydrate
    		Inducer
    Lamotrigine hydrate is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine hydrate selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine hydrate can be used for the research of epilepsy, focal seizure, et al.
    Lamotrigine hydrate
  • HY-12054A
    Hesperadin hydrochloride
    		Inhibitor
    Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC50 of 250 nM.
    Hesperadin hydrochloride
  • HY-13777B
    Zoledronic acid disodium tetrahydrate
    		Inducer
    Zoledronic Acid (Zoledronate) disodium tetrahydrate is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid disodium tetrahydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid disodium tetrahydrate also has anti-cancer effects.
    Zoledronic acid disodium tetrahydrate
  • HY-10341B
    Fasudil hydrochloride semihydrate
    		Inducer
    Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca2+ channel antagonist and vasodilator.
    Fasudil hydrochloride semihydrate
  • HY-B0338S
    Rimantadine-d4 hydrochloride
    		Inducer ≥99.0%
    Rimantadine-d4 (hydrochloride) is the deuterium labeled Rimantadine hydrochloride. Rimantadine is an orally active inhibitor for M2 protein, that blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity.
    Rimantadine-d<sub>4</sub> hydrochloride
  • HY-125465
    SLLN-15
    SLLN-15 is an oral active, selective and potent enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
    SLLN-15
  • HY-130639
    Thalidomide-NH-C4-NH-Boc
    		Inducer 99.64%
    Thalidomide-NH-C4-NH-Boc (compound 15) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-C4-NH-Boc
  • HY-108876
    Daunorubicin citrate
    		Inducer
    Daunorubicin (Daunomycin) citrate is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin citrate inhibits DNA and RNA synthesis. Daunorubicin citrate is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin citrate is also an anthracycline antibiotic. Daunorubicin citrate can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin citrate
Cat. No. Product Name / Synonyms Application Reactivity
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