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-10158S
    Bosutinib-d8
    		Inducer ≥99.0%
    Bosutinib-d8 is a deuterium labeled Bosutinib. Bosutinib is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively[1][2].
    Bosutinib-d<sub>8</sub>
  • HY-N4232
    Clematichinenoside AR
    		Inducer ≥99.0%
    Clematichinenoside AR is a major active ingredient that could be extracted from the traditional Chinese herb Clematis chinensis and has potent pharmacological effects on various diseases, including atherosclerosis (AS).
    Clematichinenoside AR
  • HY-17538S
    ZLN005-d4
    		99.52%
    ZLN005-d4 is deuterium labeled ZLN005. ZLN005 is a potent activator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α)[1].
    ZLN005-d<sub>4</sub>
  • HY-141887
    Thalidomide-O-C6-NHBoc
    		Inducer
    Thalidomide-O-C6-NHBoc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-C6-NHBoc
  • HY-10208S
    Pazopanib-d6
    		Inducer ≥98.0%
    Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib-d<sub>6</sub>
  • HY-12678S
    Entrectinib-d4
    		Inhibitor
    Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.
    Entrectinib-d<sub>4</sub>
  • HY-18085AS
    Quercetin-d3 hydrate
    		Inducer
    Quercetin-d3 hydrate is a deuterium labeled Quercetin hydrate (HY-18085A), a flavonoid which can stimulate recombinant SIRT1 and also a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
    Quercetin-d<sub>3</sub> hydrate
  • HY-15030R
    Naproxen (Standard)
    		Inducer
    Naproxen (Standard) is the analytical standard of Naproxen. This product is intended for research and analytical applications. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
    Naproxen (Standard)
  • HY-15448S
    Tezacaftor-d4
    		Inducer
    Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface.
    Tezacaftor-d<sub>4</sub>
  • HY-10255AS
    Sunitinib-d10
    		Inducer 99.89%
    Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
    Sunitinib-d<sub>10</sub>
  • HY-140055
    Thalidomide-PEG4-Propargyl
    		Inducer
    Thalidomide-PEG4-Propargyl is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-PEG4-Propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Thalidomide-PEG4-Propargyl
  • HY-13955S3
    Telmisartan-d7
    		Inducer
    Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
    Telmisartan-d<sub>7</sub>
  • HY-12047S
    Ponatinib-d8
    		Inducer 99.91%
    Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
    Ponatinib-d<sub>8</sub>
  • HY-12053
    Vinorelbine
    		Inducer
    Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
    Vinorelbine
  • HY-13605S
    Cytarabine-d2
    		Inducer ≥98.0%
    Cytarabine-d2 is the deuterium labeled Cytarabine. Cytarabine, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. Cytarabine has antiviral effects against HSV[1][2].
    Cytarabine-d<sub>2</sub>
  • HY-13677S1
    6-Mercaptopurine-13C2,15N
    		Inhibitor
    6-Mercaptopurine-13C2,15N is the 13C- and 15N-labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent.
    6-Mercaptopurine-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-103613
    Thalidomide-O-amido-C4-NH2 TFA
    		Inducer 99.92%
    Thalidomide-O-amido-C4-NH2 TFA (Cereblon Ligand-Linker Conjugates 6 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-amido-C4-NH2 TFA
  • HY-138788A
    Thalidomide-Piperazine-PEG2-NH2 diTFA
    		Inducer 99.73%
    Thalidomide-Piperazine-PEG2-NH2 diTFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-Piperazine-PEG2-NH2 diTFA
  • HY-14171S
    Bexarotene-d4
    		Inducer 99.11%
    Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
    Bexarotene-d<sub>4</sub>
  • HY-13017A
    Ivacaftor benzenesulfonate
    Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
    Ivacaftor benzenesulfonate
Cat. No. Product Name / Synonyms Application Reactivity
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