1. Signaling Pathways
  2. Autophagy
  3. Autophagy

Autophagy

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-B0178AS2
    Guanidine-13C hydrochloride
    Guanidine-13C hydrochloride (Guanidinium-13C chloride) is the 13C-labeled Guanidine hydrochloride (HY-B0178A). Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins.
    Guanidine-<sup>13</sup>C hydrochloride
  • HY-W712932
    Chenodeoxycholic Acid-d7
    Chenodeoxycholic Acid-d7 (CDCA-d7) is the deuterium labeled Chenodeoxycholic Acid (HY-76847). Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d<sub>7</sub>
  • HY-10261AS
    Afatinib-d6 dimaleate
    Inducer
    Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
    Afatinib-d<sub>6</sub> dimaleate
  • HY-14664DS
    (3S,5R)-Fluvastatin-d6
    Inducer
    (3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive?HMG-CoA reductase?inhibitor with an IC50?of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
    (3S,5R)-Fluvastatin-d<sub>6</sub>
  • HY-16562S2
    Irinotecan-13C6
    Inducer
    Irinotecan-13C6 ((+)-Irinotecan-13C6) is the 13C-labeled Irinotecan (HY-16562). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan-<sup>13</sup>C<sub>6</sub>
  • HY-12515AS1
    Nicardipine-13C,d3 hydrochloride
    Inducer
    Nicardipine-13C,d3 hydrochloride (YC-93-13C,d3) is the deuterium and 13C-labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
    Nicardipine-<sup>13</sup>C,d<sub>3</sub> hydrochloride
  • HY-176149
    Fluoxetine-Conjugated Platinum(IV) prodrug-1
    Inducer
    Fluoxetine-Conjugated Platinum(IV) prodrug-1 (Compound 8) is an eEF2K inhibitor. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits cancer cell proliferation, induces DNA damage, cell cycle arrest at S phase and apoptosis. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces ROS accumulation and mitochondrial dysfunction. Fluoxetine-Conjugated Platinum(IV) prodrug-1 inhibits TNBC cell migration and invasion by inhibiting MMP-2 activity. Fluoxetine-Conjugated Platinum(IV) prodrug-1 induces autophagy in TNBC cells by activating AMPK. Fluoxetine-Conjugated Platinum(IV) prodrug-1 has antitumor activity and activates immunosuppression in the 4T1-Luc mouse model. Fluoxetine-Conjugated Platinum(IV) prodrug-1 can be used in triple-negative breast cancer (TNBC) research.
    Fluoxetine-Conjugated Platinum(IV) prodrug-1
  • HY-14649S5
    Retinoic acid-d3
    Retinoic acid-d3 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
    Retinoic acid-d<sub>3</sub>
  • HY-10260S1
    Vandetanib-d4
    Inducer
    Vandetanib-d4 is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
    Vandetanib-d<sub>4</sub>
  • HY-N0716AR
    Berberine hemisulfate (Standard)
    Inducer
    Berberine (hemisulfate) (Standard) is the analytical standard of Berberine (hemisulfate). This product is intended for research and analytical applications. Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.
    Berberine hemisulfate (Standard)
  • HY-149573
    Thalidomide-4-O-C11-NH2 hydrochloride
    Inducer 99.94%
    Thalidomide-4-O-C11-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C11-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C11-NH2 hydrochloride
  • HY-B0309S1
    Felodipine-d5
    Inducer
    Felodipine-d5 is deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
    Felodipine-d<sub>5</sub>
  • HY-13271AG
    Tubastatin A (GMP)
    Inducer
    Tubastatin A (GMP) is the Tubastatin A (HY-13271A) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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 (GMP)
  • HY-W700643
    Di-N-desethyl amiodarone hydrochloride
    Inducer
    Di-N-desethyl Amiodarone hydrochloride is a metabolite of Amiodarone (HY-14187). Di-N-desethyl Amiodarone hydrochloride is a strong inhibitor of the respiratory chain.
    Di-N-desethyl amiodarone hydrochloride
  • HY-P992056
    Anti-Human/Mouse LY6E Antibody (9B12)
    Anti-Human/Mouse LY6E Antibody (9B12) is a high-affinity, multi-target antibody that binds specifically to LY6E. Anti-Human/Mouse LY6E Antibody (9B12) binds specifically to cell-surface LY6E and enters lysosomes via lipid raft-dependent endocytosis, thereby effectively inhibiting the growth of various LY6E-expressing solid tumors (such as breast cancer and lung cancer) in both in vitro and in vivo models. Anti-Human/Mouse LY6E Antibody (9B12) exerts a dual mechanism of action: on one hand, it blocks the interaction between PILRα and CD8α, specifically reduces the survival rate of peripheral CD8+ T cells and induces their activation, breaking the state of cellular quiescence; on the other hand, it recognizes and immunoprecipitates IDE under both non-denaturing and denaturing conditions, which is applicable to studies on the subcellular localization and protein interactions of IDE. The regulatory effect of Anti-Human/Mouse LY6E Antibody (9B12) on CD8+ T cells strictly depends on the presence of PILRα, and it does not affect CD4+ T cells or T cell development in the thymus, exhibiting high specificity.
    Anti-Human/Mouse LY6E Antibody (9B12)
  • HY-169022
    4-FPBUA
    Inducer
    4-FPBUA is a semisynthetic analog of usnic acid (HY-W015883) that can enhance cellular blood-brain barrier (BBB) function and increase the transport of Amyloid β (Aβ) across monolayer cells. 4-FPBUA is also an inhibitor of mTOR, capable of enhancing cellular Autophagy, thereby reversing BBB disruption in vivo and being utilized in research for Alzheimer's disease.
    4-FPBUA
  • HY-172201
    NF-κB-IN-19
    Inducer
    NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity.
    NF-κB-IN-19
  • HY-W654256
    Matrine-d3
    Matrine-d3 (Matridin-d3) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).
    Matrine-d<sub>3</sub>
  • HY-124896
    Bonannione A
    Inducer 98%
    Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity.
    Bonannione A
  • HY-10211S
    Tanespimycin-d5
    Tanespimycin-d5 (17-AAG-d5; NSC 330507-d5; CP 127374-d5) is the deuterium labeled Tanespimycin (HY-10211). Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
    Tanespimycin-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity