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-161205
    Thalidomide-PIP-(R)C-pyrrolidine-boc
    		Inducer
    Thalidomide-PIP-(R)C-pyrrolidine-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-PIP-(R)C-pyrrolidine-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-PIP-(R)C-pyrrolidine-boc
  • HY-156160
    Thalidomide-NH-C10-NH2 hydrochloride
    		Inducer
    Thalidomide-NH-C10-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-NH-C10-NH2 hydrochloride
  • HY-161184
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
    		Inducer
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-piperidine-C-piperazine-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
  • HY-162310
    Anticancer agent 193
    		Inducer
    Anticancer agent 193 (compound D3-3) is an inducer of ferritinophagy, eventually triggering ferroptosis. Anticancer agent 193 induces the production of lipid ROS, and significantly promoted colorectal cancer cells to release the ferrous ion in an autophagy-dependent manner.
    Anticancer agent 193
  • HY-181009
    HDAC-IN-98
    		Inducer
    HDAC-IN-98 is a HDAC1, HDAC2, HDAC3 inhibitor (one of the most selective class I HDAC inhibitors) with human IC50 values of 41.2 nM, 52.5 nM, and 74.3 nM respectively. HDAC-IN-98 induces H3K9 acetylation, p21 upregulation, G2/M arrest, cell apoptosis, has strong antiproliferative effects in colorectal cancer cells, low toxicity in healthy colon epithelium, modulates short-term in vitro effects via autophagy, and shows strong antitumor efficacy in vivo in the chorioallantoic membrane model (CAM) assay. HDAC-IN-98 can be used for the research of colorectal cancer.
    HDAC-IN-98
  • HY-19980G
    Eprenetapopt (GMP)
    		Inducer
    Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
    Eprenetapopt (GMP)
  • HY-W768895
    Sanguinarine chloride-13C,d3
    Sanguinarine chloride-13C,d3 (Sanguinarin chloride-13C,d3) is the deuterium labeled Sanguinarine chloride (HY-N0052A). Sanguinarine (Sanguinarin) chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
    Sanguinarine chloride-<sup>13</sup>C,d<sub>3</sub>
  • HY-13704S2
    SN-38-13C6
    		Inducer
    SN-38-13C6 (7-Ethyl-10-hydroxycamptothecin-13C6) is the 13C-labeled SN-38 (HY-13704). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
    SN-38-<sup>13</sup>C<sub>6</sub>
  • HY-N10408
    Tripchlorolide
    		Inducer
    Tripchlorolide is a neuroprotective agent that can be found in Tripterygium wilfordii. Tripchlorolide prevents tumor growth by inducing apoptosis and autophagy. Tripchlorolide improves cognitive deficits in Alzheimer's disease.
    Tripchlorolide
  • HY-169824
    TRPML modulator 1
    		Inducer
    TRPML modulator 1 (compound A12) is a TRPML modulator that promotes autophagy. TRPML modulator 1 AC50 in the TFEB test is less than 2 mM.
    TRPML modulator 1
  • HY-W768912
    Paclitaxel-13C6
    Paclitaxel-13C6 is the 13C-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes?tubulin?polymerization. Paclitaxel can cause both mitotic arrest and?apoptotic?cell death. Paclitaxel also induces?autophagy.
    Paclitaxel-<sup>13</sup>C<sub>6</sub>
  • HY-10961S8
    Momelotinib-d4 dihydrochloride hydrate
    Momelotinib-d4 (CYT387-d4) dihydrochloride hydrate is a deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50s of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
    Momelotinib-d<sub>4</sub> dihydrochloride hydrate
  • HY-W016409R
    Ethyl 3,4-dihydroxybenzoate (Standard)
    		Inducer
    Ethyl 3,4-dihydroxybenzoate (Standard) (Protocatechuic acid ethyl ester (Standard)) is the analytical standard of Ethyl 3,4-dihydroxybenzoate (HY-W016409). This product is intended for research and analytical applications. Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema.
    Ethyl 3,4-dihydroxybenzoate (Standard)
  • HY-121726
    3HOI-BA-01
    		Inducer
    3HOI-BA-01 is amTORinhibitor.3HOI-BA-01reduces infarct size and inducedautophagyin a murine myocardial ischemia/reperfusion injury model.
    3HOI-BA-01
  • HY-N0656AR
    (+)-Usnic acid (Standard)
    		Inducer
    (+)-Usnic acid (Standard) is the analytical standard of (+)-Usnic acid. This product is intended for research and analytical applications. (+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity. (+)-Usnic acid possesses antimicrobial activity against a number of planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium.
    (+)-Usnic acid (Standard)
  • HY-16562AR
    Irinotecan hydrochloride (Standard)
    		Inducer
    Irinotecan (hydrochloride) (Standard) is the analytical standard of Irinotecan (hydrochloride). This product is intended for research and analytical applications. Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.
    Irinotecan hydrochloride (Standard)
  • HY-W744064
    Diethylstilbestrol-d4
    Diethylstilbestrol-d4 is the deuterium labeled Diethylstilbestrol (HY-14598). Diethylstilbestrol is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and?Apoptosis?of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte?Autophagy?Diethylstilbestrol is a?11β-hydroxysteroid dehydrogenase 2 (HSD11B2)?inhibitor.
    Diethylstilbestrol-d<sub>4</sub>
  • HY-138851
    Thalidomide-NH-amido-C5-NH2
    		Inducer
    Thalidomide-NH-amido-C5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-C5-NH2
  • HY-176239
    PROTAC PI3Kδ degrader-1
    		Inducer
    PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model. Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
    PROTAC PI3Kδ degrader-1
  • HY-17577R
    Berberine chloride hydrate (Standard)
    		Modulator
    Berberine (chloride hydrate) (Standard) is the analytical standard of Berberine (chloride hydrate). This product is intended for research and analytical applications. Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid that acts as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
    Berberine chloride hydrate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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