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-B0338S
    Rimantadine-d4 hydrochloride
    		Inducer 99.79%
    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-131889
    Thalidomide-O-C5-acid
    		Inducer
    Thalidomide-O-C5-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-C5-acid
  • HY-138781
    Thalidomide-Piperazine-PEG2-COOH
    		Inducer 99.79%
    Thalidomide-Piperazine-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-Piperazine-PEG2-COOH
  • HY-W031727S
    Hydroxychloroquine-d4-1 sulfate
    		Inhibitor ≥98.0%
    Hydroxychloroquine-d4-1 (sulfate) is the deuterium labeled Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
    Hydroxychloroquine-d<sub>4</sub>-1 sulfate
  • HY-B0006S
    Carvedilol-d3
    		Inducer 99.00%
    Carvedilol-d3 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
    Carvedilol-d<sub>3</sub>
  • HY-115412
    Vorinostat-d5
    		Inducer 99.0%
    Vorinostat-d5 (SAHA-d5) is the deuterium labeled Vorinostat. Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
    Vorinostat-d5
  • HY-14249S
    Bicalutamide-d4
    		Inducer
    Bicalutamide-d4 is the deuterium labeled Bicalutamide. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
    Bicalutamide-d<sub>4</sub>
  • HY-14188S
    Amiodarone-d4 hydrochloride
    		Inducer 99.58%
    Amiodarone-d4 (hydrochloride) is the deuterium labeled Amiodarone hydrochloride. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ～45 nM. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias.
    Amiodarone-d<sub>4</sub> hydrochloride
  • HY-13768S1
    Topotecan-d6
    		Inducer
    Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87.
    Topotecan-d<sub>6</sub>
  • HY-13955S
    Telmisartan-d3
    		Inducer 99.77%
    Telmisartan-d3 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
    Telmisartan-d<sub>3</sub>
  • HY-B0863S2
    Glyphosate-d2-1
    		99.89%
    Glyphosate-d2-1 is the deuterium labeled Glyphosate. Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants.
    Glyphosate-d<sub>2</sub>-1
  • HY-10261S
    Afatinib-d6
    		Inducer 99.0%
    Afatinib-d6 (BIBW 2992-d6) is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor.
    Afatinib-d<sub>6</sub>
  • HY-124726
    Aumitin
    		Inhibitor 99.78%
    Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively.
    Aumitin
  • HY-17393S
    Carboplatin-d4
    		Inducer 99.0%
    Carboplatin-d4 is the deuterium labeled Carboplatin. Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.
    Carboplatin-d<sub>4</sub>
  • HY-N2359
    Chelerythrine
    		Inducer
    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
    Chelerythrine
  • HY-B0365AS
    Memantine-d6 hydrochloride
    		Inducer 99.83%
    Memantine-d6 (hydrochloride) is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Kis of 0.51 nM and 94.9 μM, respectively.
    Memantine-d<sub>6</sub> hydrochloride
  • HY-141013
    Thalidomide-O-amido-PEG4-propargyl
    		Inducer 98.0%
    Thalidomide-O-amido-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Thalidomide-O-amido-PEG4-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Thalidomide-O-amido-PEG4-propargyl
  • HY-14187S
    Amiodarone-d10 hydrochloride
    		Inducer 98.81%
    Amiodarone-d10 (hydrochloride) is the deuterium labeled Amiodarone. Amiodarone hydrochloride is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.
    Amiodarone-d<sub>10</sub> hydrochloride
  • HY-105037
    Forigerimod
    		Inhibitor
    Forigerimod (IPP-201101) is a CD4 T-cell modulator. Forigerimod is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
    Forigerimod
  • HY-139207
    Glucosamine sulfate potassium chloride
    Glucosamine sulfate potassium chloride is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine sulfate potassium chloride also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
    Glucosamine sulfate potassium chloride
Cat. No. Product Name / Synonyms Application Reactivity
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