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-10284S3
    Linagliptin-d3-1
    		Inducer
    Linagliptin-d3-1 (BI 1356-d3-1) is the deuterium labeled Linagliptin (HY-10284). Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
    Linagliptin-d<sub>3</sub>-1
  • HY-10585S3
    Valproic acid-d4 sodium
    		Inducer
    Valproic acid-d4 (sodium) 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.
    Valproic acid-d<sub>4</sub> sodium
  • HY-W050000R
    OR-1855 (Standard)
    		Inhibitor
    Tanshinone IIA sulfonate (sodium) (Standard) is the analytical standard of Tanshinone IIA sulfonate (sodium). This product is intended for research and analytical applications. Tanshinone IIA sulfonate (sodium) is a derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca2+ entry (SOCE), and is used to treat cardiovascular disorders.
    OR-1855 (Standard)
  • HY-N0006S
    Demethoxycurcumin-d7
    		Inducer
    Demethoxycurcumin-d7 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin(Curcumin II), a major active curcuminoid, possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.
    Demethoxycurcumin-d<sub>7</sub>
  • HY-B0450R
    Ciclopirox (Standard)
    		Inducer
    Ciclopirox (Standard) is the analytical standard of Ciclopirox. This product is intended for research and analytical applications. Ciclopirox (HOE296b) is a synthetic and orally active antifungal agent that can be used for superficial mycoses reseaech. Ciclopirox olamine has a very broad spectrum of activity and inhibits dermatophytes, yeasts, molds, and many Gram-positive and Gram-negative species pathogenic. Ciclopirox also has anticancer and anti-inflammatory effect.
    Ciclopirox (Standard)
  • HY-10820AS
    Pemetrexed-d5 disodium
    		Inducer
    Pemetrexed-d5 (disodium) is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].
    Pemetrexed-d<sub>5</sub> disodium
  • HY-172094
    AMPK-IN-6
    		Inhibitor
    AMPK-IN-6 (compound 13a) is potent AMPK inhibitor with an IC50 value of 0.093 µM. AMPK-IN-6 induces apoptosis and inhibits autophagy. AMPK-IN-6 shows antiproliferative activity. AMPK-IN-6 has the potential for the research of pulmonary arterial hypertension.
    AMPK-IN-6
  • HY-15373R
    Fenretinide (Standard)
    		Inducer
    Fenretinide (Standard) is the analytical standard of Fenretinide. This product is intended for research and analytical applications. Fenretinide (4-HPR) is a synthetic retinoid deriverative, binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.
    Fenretinide (Standard)
  • HY-134985
    Thalidomide-NH-PEG1-NH2
    		Inducer
    Thalidomide-NH-PEG1-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-PEG1-NH2
  • HY-162147
    Nur77 modulator 3
    		99.01%
    Nur77 modulator 3 (9e) can bind to Nur77 and inhibit TGF-β1-induced α-SMA and COLA1 expression in a Nur77-dependent manner. Nur77 modulator 3 induces Nur77 expression and enhances autophagic flux by inhibiting the mTORC1 signaling pathway in vitro and in vivo. Nur77 modulator 3 blocks the progression of hepatic fibrosis.
    Nur77 modulator 3
  • HY-13551B
    Amsacrine (gluconate)
    		Inducer
    Amsacrine gluconate is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine (gluconate)
  • HY-N3883
    Euxanthone
    		Inducer
    Euxanthone, a xanthone derivative, attenuates Aβ1-42-induced oxidative stress and apoptosis by triggering autophagy. Euxanthone exhibits anti-neoplastic and neuroprotective activities.
    Euxanthone
  • HY-17379R
    Atorvastatin (hemicalcium salt) (Standard)
    		Inducer
    Atorvastatin (hemicalcium salt) (Standard) is the analytical standard of Atorvastatin (hemicalcium salt). This product is intended for research and analytical applications. Atorvastatin hemicalcium salt (CI-981) is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium salt inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
    Atorvastatin (hemicalcium salt) (Standard)
  • HY-103086
    INU-152
    INU-152 is a potent and selective B-Raf inhibitor. INU-152 reduces tumor cell proliferation, enhances autophagy, and induces apoptosis by inhibiting B-Raf activity. INU-152 exhibits significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3). INU-152 can be utilized in cancer research.
    INU-152
  • HY-135533
    Chromomycin A2
    		Inducer
    Chromomycin A2 (Aburamycin A) has cytotoxicity and induces autophagy. Chromomycin A2 has anti-tumor activity and can be used in cancer research.
    Chromomycin A2
  • HY-170667
    Autophagy activator-1
    		Activator
    Autophagy activator-1 (Compound B2) is an autophagy activator Autophagy. Activator-1 ultimately leads to the activation of autophagy by downregulating key members of the HSP70 family and activating the unfolded protein response.
    Autophagy activator-1
  • HY-17401S
    Ranolazine-d8 dihydrochloride
    		Inducer ≥99.0%
    Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].
    Ranolazine-d<sub>8</sub> dihydrochloride
  • HY-103691
    ARN5187
    		Inhibitor
    ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis.
    ARN5187
  • HY-159483
    SelB-1
    		Inducer
    SelB-1 serves as a dual inhibitor for Topoisomerase I/II. SelB-1 possesses anticancer activity and can be utilized in the research of prostate cancer and colon cancer. Furthermore, SelB-1 is also capable of inducing autophagy gene expression and lipid peroxidation, while simultaneously reducing the level of GSH.
    SelB-1
  • HY-17589S1
    Chloroquine-d4 phosphate
    		Inhibitor
    Chloroquine-d4 (phosphate) is the deuterium labeled Chloroquine phosphate. Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
    Chloroquine-d<sub>4</sub> phosphate
Cat. No. Product Name / Synonyms Application Reactivity
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