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-W145436
    Thalidomide-Piperazine 5-fluoride hydrochloride
    		Inducer 98.91%
    Thalidomide-Piperazine 5-fluoride hydrochloride is a derivative of cereblon (CRBN) inhibitor Thalidomide (HY-14658), which can be used as ligands for E3 ubiquitin ligase (Ligands for E3 Ligase) for PROTACs Synthesis.
    Thalidomide-Piperazine 5-fluoride hydrochloride
  • HY-103614
    Thalidomide-O-amido-C8-NH2 TFA
    		Inducer 99.43%
    Thalidomide-O-amido-C8-NH2 TFA (Cereblon Ligand -Linker Conjugates 2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-amido-C8-NH2 TFA
  • HY-113636
    Kazinol A
    		Inducer
    Kazinol A induces cytotoxic effects in human bladder cancer cells, including the cisplatin-resistant T24R2.
    Kazinol A
  • HY-134807
    Indophagolin
    		Inhibitor 98.05%
    Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.
    Indophagolin
  • HY-132971
    Thalidomide-piperazine hydrochloride
    		Inducer 98.27%
    Thalidomide-piperazine hydrochloride has the potential for the research of leprosy and multiple myeloma. Thalidomide-piperazine hydrochloride used as a tool in developmental biology leads to important discoveries in the biochemical pathways of limb development.
    Thalidomide-piperazine hydrochloride
  • HY-14374
    GPP78
    		Inducer ≥99.0%
    GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.
    GPP78
  • HY-W007355S1
    Skatole-d8
    		98.50%
    Skatole-d8 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38[1].
    Skatole-d<sub>8</sub>
  • HY-10162S3
    Olaparib-d4-1
    		Inducer 98.59%
    Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
    Olaparib-d<sub>4</sub>-1
  • HY-17508S1
    Clarithromycin-d3
    		Inhibitor 99.90%
    Clarithromycin-d3 is the deuterium labeled Clarithromycin (HY-17508). Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.
    Clarithromycin-d<sub>3</sub>
  • HY-10284S
    Linagliptin-d4
    		Inducer 99.62%
    Linagliptin-d4 is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Linagliptin-d<sub>4</sub>
  • HY-B0863R
    Glyphosate (Standard)
    		Inducer
    Glyphosate (Standard) is the analytical standard of Glyphosate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0197R
    Baicalin (Standard)
    		Inducer
    Baicalin (Standard) is the analytical standard of Baicalin. This product is intended for research and analytical applications. Baicalin, as a flavonoid glycoside, is an allosteric carnitine palmityl transferase 1 (CPT1) activator. Baicalin reduces the expression of NF-κB.
    Baicalin (Standard)
  • HY-N1201R
    Apigenin (Standard)
    		Inducer
    Apigenin (Standard) is the analytical standard of Apigenin. This product is intended for research and analytical applications. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
    Apigenin (Standard)
  • HY-N0817
    Polyphyllin G
    		Inhibitor
    Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs). Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy.
    Polyphyllin G
  • HY-N0136S1
    (±)-Taxifolin-13C3
    		Inhibitor 99.63%
    (±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
    (±)-Taxifolin-<sup>13</sup>C<sub>3</sub>
  • HY-103611
    Thalidomide-O-amido-PEG3-C2-NH2 TFA
    		Inducer 99.55%
    Thalidomide-O-amido-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
    Thalidomide-O-amido-PEG3-C2-NH2 TFA
  • HY-146349
    PROTAC EGFR degrader 4
    		99.70%
    PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
    PROTAC EGFR degrader 4
  • HY-169369
    TRAP-1
    		99.69%
    TRAP-1 (XJZ-06-462) is ap53 transcriptional activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. TRAP-1 rapidly upregulates p21 and other p53 target genes in pancreatic cell lines with p53Y220C. TRAP-1 inhibits cell proliferation, with IC50 values of 3.94 and 0.531 μM in BxPC-3 and A549 cells, respectively. TRAP-1 regulates autophagy in lung cancer cells and offers protective effects against oxidative stress and cell apoptosis.
    TRAP-1
  • HY-NP131
    Recombinant Humanized Type III Collagen (10.4kDa)
    		Inhibitor
    Recombinant Humanized Type III Collagen 10.4kDa is a novel biomaterial that have anticancer effects. Recombinant Humanized Type III Collagen 10.4kDa activates discoidin domain receptor 1 (DDR1), and thus inhibits autophagy, proliferation, and migration of cancer cells, and induces apoptosis.
    Recombinant Humanized Type III Collagen (10.4kDa)
  • HY-144636
    Atg4B-IN-2
    		Inhibitor 98.03%
    Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition.
    Atg4B-IN-2
Cat. No. Product Name / Synonyms Application Reactivity
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