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-10328
    Neflamapimod
    		99.32%
    Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
    Neflamapimod
  • HY-101296
    PD-166866
    		Inducer 99.75%
    PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.
    PD-166866
  • HY-B1140
    Diazoxide
    		Inducer 99.99%
    Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
    Diazoxide
  • HY-101180
    C2 Ceramide
    		Inducer 99.85%
    C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation, autophagy and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
    C2 Ceramide
  • HY-N0031
    Plantamajoside
    		Activator 99.80%
    Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects.
    Plantamajoside
  • HY-50514
    AT9283
    		Inducer 99.67%
    AT9283 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 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
    AT9283
  • HY-15888
    PTC-209
    		Inducer 99.76%
    PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment.
    PTC-209
  • HY-103319
    Calmidazolium chloride
    		99.94%
    Calmidazolium chloride (R 24571) is a calmodulin antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to calmodulin with a Kd of 3 nM.
    Calmidazolium chloride
  • HY-N0370
    Bergapten
    		Inducer 99.96%
    Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
    Bergapten
  • HY-N1435
    Oroxin B
    		99.39%
    Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent. Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT. Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells.
    Oroxin B
  • HY-13777A
    Zoledronic acid monohydrate
    		Inducer 99.88%
    Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.
    Zoledronic acid monohydrate
  • HY-N2581
    Phytic acid sodium salt
    		Activator
    Phytic acid (myo-Inositol; hexakis dihydrogen phosphate; Inositol hexaphosphate) sodium salt is an orally active compound. Phytic acid sodium salt can be derived from the seeds of legumes. Phytic acid sodium salt is a [PO4]3- storage depot and precursor for other inositol phosphates and pyrophosphates. Phytic acid sodium salt attenuates Aβ oligomers and upregulates autophagy protein. Phytic acid sodium salt can be used in cardiovascular disease, metabolic disease, nervous system disease and cancer research.
    Phytic acid sodium salt
  • HY-13252
    MK-5108
    		Inducer 99.60%
    MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM.
    MK-5108
  • HY-N2149
    Tomatidine
    		Inducer 98.0%
    Tomatidine acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine activates autophagy either in mammal cells or C elegans.
    Tomatidine
  • HY-10182G
    Laduviglusib (GMP)
    		Inducer
    Laduviglusib (CHIR-99021) (GMP) is Laduviglusib (HY-10182) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Laduviglusib is a potent, orally active and selective GSK-3α/β inhibitor.
    Laduviglusib (GMP)
  • HY-100548
    GSK621
    		Inducer 98.03%
    GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
    GSK621
  • HY-10912
    Fexaramine
    		99.20%
    Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.
    Fexaramine
  • HY-13425
    Deguelin
    		Inducer 99.20%
    Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
    Deguelin
  • HY-N0674
    Dehydrocorydaline
    		99.77%
    Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
    Dehydrocorydaline
  • HY-50909
    Perifosine
    		Inducer 99.91%
    Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
    Perifosine
Cat. No. Product Name / Synonyms Application Reactivity
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