1. Signaling Pathways
  2. Autophagy
  3. Autophagy

Autophagy

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-B0246S1
    Carbamazepine-d2
    Inducer
    Carbamazepine-d2 is the deuterium labeled Carbamazepine. Carbamazepine, a sodium channel blocker, is an anticonvulsant agent.
    Carbamazepine-d<sub>2</sub>
  • HY-15206S
    Glyburide-d11
    Inducer
    Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
    Glyburide-d<sub>11</sub>
  • HY-14393S
    Emodin-d4
    Inhibitor
    Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
    Emodin-d<sub>4</sub>
  • HY-15025S1
    Sildenafil-d8
    Inducer
    Sildenafil-d8 is the deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM[1][2].
    Sildenafil-d<sub>8</sub>
  • HY-15388S
    Tazarotene-d8
    Tazarotene-d8 is the deuterium labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris[1][2].
    Tazarotene-d<sub>8</sub>
  • HY-14266S
    Dapivirine-d11
    Inducer
    Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
    Dapivirine-d<sub>11</sub>
  • HY-15296S
    Cabergoline-d5
    Inducer
    Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].
    Cabergoline-d<sub>5</sub>
  • HY-10882S
    Clotrimazole-d5
    Inhibitor
    Clotrimazole-d5 is the deuterium labeled Clotrimazole. Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity[1][2].
    Clotrimazole-d<sub>5</sub>
  • HY-115570A
    (Z/E)-GW406108X
    Inhibitor
    (Z/E)-GW406108X is a mixture of different configurations of GW406108X (HY-115570). GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM.
    (Z/E)-GW406108X
  • HY-100587R
    D-Glutamine (Standard)
    Inducer
    D-Glutamine (Standard) is the analytical standard of D-Glutamine. This product is intended for research and analytical applications. D-Glutamine is a cell-permeable D type stereoisomer of Glutamine.
    D-Glutamine (Standard)
  • HY-13683S1
    Mifepristone-13C,d3
    Inducer
    Mifepristone-13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1]. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Mifepristone-<sup>13</sup>C,d<sub>3</sub>
  • HY-B0084S2
    Dienogest-d6
    Inducer 99.92%
    Dienogest-d6 is deuterium labeled Dienogest (HY-B0084). Dienogest is an orally active progesterone receptor agonist that can be used in the study of endometriosis.
    Dienogest-d<sub>6</sub>
  • HY-Y1269D
    Ammonium chloride, for molecular biology
    Inhibitor
    Ammonium chloride, for molecular biology is ammonium chloride that can be used for molecular biology research. Ammonium chloride can be used as a heteropolar compound to regulate pH value, which can cause intracellular alkalination and metabolic acidosis, thus affecting the activity of enzymes and affecting the process of biological systems. Ammonium chloride is an autophagy inhibitor. Ammonium chloride is also a lysosome inhibitor.
    Ammonium chloride, for molecular biology
  • HY-P0214
    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
  • HY-118326
    MRT 68601
    MRT 68601 is a potent TBK1 inhibitor with the activity of inhibiting autophagosome formation in lung cancer cells. MRT 68601 may have potential effects against targets associated with host-dependent factors identified in SARS-CoV-2 infection. The drug targets involved in MRT 68601 are related to existing FDA-approved drugs and compounds in clinical trials, which can provide support for the development of broad-spectrum antiviral therapies.
    MRT 68601
  • HY-W031727S1
    Hydroxychloroquine-d5
    Hydroxychloroquine-d5 is the deuterium labeled Hydroxychloroquine[1]. 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[2][3][4].
    Hydroxychloroquine-d<sub>5</sub>
  • HY-N0560R
    Oroxylin A (Standard)
    Inducer
    Oroxylin A (Standard) is the analytical standard of Oroxylin A. This product is intended for research and analytical applications. Oroxylin A is an active flavonoid compound with strong anti-cancer effects. Oroxylin A inhibits the IL-6/STAT3 pathway and NF-κB signaling, inhibits cell proliferation and induces apoptosis. Oroxylin A inhibits colitis-related carcinogenesis.
    Oroxylin A (Standard)
  • HY-119327
    Butylate
    Inducer
    Butylate is a compound involved in platelet research. Platelet activation can cause autophagy, which is partly mediated by the AMPK-MTOR pathway and is related to sphingolipid metabolism. Butylate mentioned in the study may be a tool or control substance for studying related metabolic processes.
    Butylate
  • HY-B0165S
    Pravastatin-d9 sodium
    Activator
    Pravastatin-d9 sodium is deuterated labeled Pravastatin (HY-B0165). Pravastatin (CS-514) is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
    Pravastatin-d<sub>9</sub> sodium
  • HY-172813
    Vancomycin prodrug
    Vancomycin prodrug (compound 13c) is a Vancomycin (HY-B0671) prodrug. Vancomycin prodrug shows antibacterial effect with MICs of 0.78 μM, 0.78 μM, 1.56 μM for S. aureus 330041, MRSA USA 300 and MRSA 3390, respectively. Vancomycin prodrug has the ability to quickly bind to Cys-34 residue of plasma. Vancomycin prodrug exhibits a good therapeutic effect on MRSA USA300 infected mice similar to Vancomycin. Vancomycin prodrug, an albumin-binding acid-sensitive prodrug, effectively reduces Vancomycin’s nephrotoxicity while maintaining its efficacy for Gram-positive bacterial infections.
    Vancomycin prodrug
Cat. No. Product Name / Synonyms Application Reactivity