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-114405
    SJFδ
    SJFδ is a 10-atom linker PROTAC based on von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ.
    SJFδ
  • HY-140240
    Amino-PEG6-Thalidomide
    		Inducer
    Amino-PEG6-Thalidomide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Amino-PEG6-Thalidomide
  • HY-152965
    Biotin-doxorubicin
    		Inducer
    Biotin-doxorubicin is a Biotin-labeled Doxorubicin. Doxorubicin, a broad-spectrum anthracycline antibiotic, is a topoisomerase II inhibitor.
    Biotin-doxorubicin
  • HY-N3584R
    Paris saponin VII (Standard)
    		Inducer
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
    Paris saponin VII (Standard)
  • HY-151216S
    rel-Paroxetine-d4 hydrochloride
    		Inducer
    rel-Paroxetine-d4 (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].
    rel-Paroxetine-d<sub>4</sub> hydrochloride
  • HY-10260S
    Vandetanib-d6
    		Inducer
    Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
    Vandetanib-d<sub>6</sub>
  • HY-17506R
    Azithromycin (Standard)
    		Inhibitor
    Azithromycin (Standard) is the analytical standard of Azithromycin. This product is intended for research and analytical applications. Azithromycin is a macrolide antibiotic useful for the treatment of a number of bacterial infections.
    Azithromycin (Standard)
  • HY-16562S
    Irinotecan-d10
    		Inducer
    Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1].
    Irinotecan-d<sub>10</sub>
  • HY-16561S1
    Resveratrol-13C6
    		Inducer
    Resveratrol-13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
    Resveratrol-<sup>13</sup>C<sub>6</sub>
  • HY-124281
    9(R)-PAHSA
    9(R)-PAHSA is a R-enantiomer of 9-PAHSA. 9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation.
    9(R)-PAHSA
  • HY-155717
    NDBM
    NDBM is a probe and binds to tumor-specific Pim-1 kinase, releases strong fluorescence, and produces cytotoxicity, thus achieving cell screening and killing effects. NDBM can specifically target lysosomes and sensitively respond to pH. NDBM can be used to track the pH changes in the intracellular environment under conditions of autophagy and external stimulation.
    NDBM
  • HY-17502S
    Simvastatin-d11
    Simvastatin-d11 is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM[1][2].
    Simvastatin-d<sub>11</sub>
  • HY-158373
    Anticancer agent 213
    		Inducer
    Anticancer agent 213 (Compound 1) exhibits anticancer efficacy by self-assembling into micelles, depleting membran cholesterol and thus inhibiting cancer cells. Anticancer agent 213 exhibits cytotoxicity against HeLa and PC3, with IC50 of 10.3 and 13.7 μM. Anticancer agent 213 induces autophagy.
    Anticancer agent 213
  • HY-119327R
    Butylate (Standard)
    		Inducer
    Butylate (Standard) is the analytical standard of Butylate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0330R
    Momordin Ic (Standard)
    		Inducer
    Momordin Ic (Standard) is the analytical standard of Momordin Ic. This product is intended for research and analytical applications. Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl4 (HY-Y0298) induced hepatotoxicity and anti-tumor activity.
    Momordin Ic (Standard)
  • HY-168962
    HDAC-IN-88
    		Inducer
    HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC50s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC50 of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC50 of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity.
    HDAC-IN-88
  • HY-10284S1
    Linagliptin-13C,d3
    		Inducer
    Linagliptin-13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-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.
    Linagliptin-<sup>13</sup>C,d<sub>3</sub>
  • HY-15371R
    Forskolin (Standard)
    		Inducer
    Forskolin (Standard) is the analytical standard of Forskolin. This product is intended for research and analytical applications. Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
    Forskolin (Standard)
  • HY-10448S4
    Capsaicin-d7
    		Inducer
    Capsaicin-d7 is deuterated labeled Capsaicin (HY-10448). Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects.
    Capsaicin-d<sub>7</sub>
  • HY-103438A
    BIBU1361 dihydrochloride
    		Inhibitor
    BIBU1361 dihydrochloride induces apoptosis and inhibits autophagy. BIBU1361 inhibits pro-survival pathways Akt/mTOR and gp130/JAK/STAT3, and decreased levels of pro-inflammatory cytokine IL-6.
    BIBU1361 dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
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