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-17508R
    Clarithromycin (Standard)
    		Inhibitor
    Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-161586
    Chloramphenicol/BSA
    		Inducer
    Chloramphenicol/BSA is the antigen-adjuvant conjugate formed by the coupling of Chloramphenicol (HY-B0239) with Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
    Chloramphenicol/BSA
  • HY-161199
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH
    		Inducer
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH
  • HY-151914
    Antitumor agent-82
    		Inducer
    Antitumor agent-82 (compound 6g) is a potent anti-tumor agent. Antitumor agent-82 shows anti-proliferative activity. Antitumor agent-82 induces cell Autophagy by the ATG5/ATG7 signaling pathway.
    Antitumor agent-82
  • HY-139546
    Thalidomide-5-propargyne-NH2 hydrochloride
    		Inducer
    Thalidomide-5-propargyne-NH2 hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-propargyne-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-propargyne-NH2 hydrochloride
  • HY-P0215A
    Autocamtide-2-related inhibitory peptide, myristoylated TFA
    Autocamtide-2-related inhibitory peptide, myristoylated TFA is the myristoylated Autocamtide-2-related inhibitory peptide. Autocamtide-2-related inhibitory peptide is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.
    Autocamtide-2-related inhibitory peptide, myristoylated TFA
  • HY-168477
    HDAC1-IN-8
    		Inducer
    HDAC1-IN-8 (compound 5c) is a potent and selective HDAC1 inhibitor with IC50 values of 11.94, 22.95, >500 µM for HDAC1, HDAC6, HDAC8, respectively. HDAC1-IN-8 shows antiproliferative activity. HDAC1-IN-8 induces cell cycle arrest at G1 and G2/M. HDAC1-IN-8 induces autophagy. HDAC1-IN-8 shows anticancer activity and has the potential for the research of lung cancer.
    HDAC1-IN-8
  • HY-P4808
    PHF6
    		Activator
    PHF6 (VQIVYK) is a self-assembly sequence capable of initiating the full-length tau protein aggregation and is mapped to the third microtubule-binding repeat region of the tau protein.
    PHF6
  • HY-162944
    NA-Ir
    NA-Ir is a Ferroptosis inducer. NA-Ir targets mitochondrial DNA (mtDNA) and activates the cGAS-STING pathway to induce ferritinophagy (Autophagy), while also generating reactive oxygen species (ROS) through photodynamic therapy (PDT), depleting glutathione (GSH), and downregulating glutathione peroxidase 4 (GPX4), thereby triggering lipid peroxidation and Ferroptosis. NA-Ir exhibits higher anticancer activity under light exposure and selectively inhibits cancer cells with high H2S levels.
    NA-Ir
  • HY-161210
    Thalidomide-azetidine-C-PIP-C-boc
    		Inducer
    Thalidomide-azetidine-C-PIP-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-C-PIP-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-C-PIP-C-boc
  • HY-N2585
    Isodeoxyelephantopin
    		Inducer ≥98.0%
    Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
    Isodeoxyelephantopin
  • HY-B0495S4
    Lamotrigine-13C3
    		Inducer
    Lamotrigine-13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
    Lamotrigine-<sup>13</sup>C<sub>3</sub>
  • HY-B0261S1
    Meloxicam-d3-1
    		Inducer ≥98.0%
    Meloxicam-d3-1 is the deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.
    Meloxicam-d<sub>3</sub>-1
  • HY-B0923R
    Danthron (Standard)
    		Inhibitor
    Danthron (Standard) is the analytical standard of Danthron. This product is intended for research and analytical applications. Danthron is a natural product extracted from the traditional Chinese medicine Salvia miltiorrhiza Bunge. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
    Danthron (Standard)
  • HY-N3980R
    Guaiol (Standard)
    Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions[4]
    Guaiol (Standard)
  • HY-10585S4
    Valproic acid-d4-1
    		Inducer
    Valproic acid-d4-1 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
    Valproic acid-d<sub>4</sub>-1
  • HY-N0678R
    Icaritin (Standard)
    		Inducer
    Icaritin (Standard) is the analytical standard of Icaritin. This product is intended for research and analytical applications. Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC50 of 8 μM) and primary CML cells (IC50 of 13.4 μM for CML-CP and 18 μM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[3.
    Icaritin (Standard)
  • HY-161193
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc
    		Inducer
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc
  • HY-N6872R
    Actein (Standard)
    		Inducer
    Actein (Standard) is the analytical standard of Actein. This product is intended for research and analytical applications. Actein, a triterpene glycoside, shows an inhibitory effect on cancer cells, which is isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in bladder cancer. Actein has little toxicity in vivo.
    Actein (Standard)
  • HY-13417S
    AICAR-13C2,15N
    		Inhibitor
    AICAR-13C2,15N (Acadesine-13C2,15N; AICA Riboside-13C2,15N) is the 13C and 15N labeled AICAR (HY-13417). AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
    AICAR-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
Cat. No. Product Name / Synonyms Application Reactivity
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