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-161647
    Antitumor agent-156
    		Inducer
    Antitumor agent-156 (Compound 20) causes DNA damage and mitochondrial dysfunction, promotes reactive oxygen species generation, activates endoplasmic reticulum stress, and induce apoptosis, autophagy and ferroptosis. Antitumor agent-156 shows superior antitumor activity against cancer cells including Cisplatin (HY-17394) resistance cells. Antitumor agent-156 displayS good liver-targeting ability.
    Antitumor agent-156
  • HY-19312R
    3-Methyladenine (Standard)
    		Inhibitor
    3-Methyladenine (Standard) is the analytical standard of 3-Methyladenine. This product is intended for research and analytical applications. 3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.
    3-Methyladenine (Standard)
  • HY-B0003R
    Gemcitabine (hydrochloride) (Standard)
    		Inducer
    Gemcitabine (hydrochloride) (Standard) is the analytical standard of Gemcitabine (hydrochloride). This product is intended for research and analytical applications. Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis.
    Gemcitabine (hydrochloride) (Standard)
  • HY-16508S
    Ulipristal acetate-d6
    		Inducer
    Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma[1][2].
    Ulipristal acetate-d<sub>6</sub>
  • HY-114383
    ST-539
    		Inducer
    ST-539 is the inhibitor for deubiquitinase USP30 with IC50 of 0.37 μM. ST-539 promotes the ubiquitination of mitochondrial proteins, and induces mitochondrial autophagy, thereby regulating mitochondrial homeostasis. ST-539 can be used in research of neurodegenerative diseases.
    ST-539
  • HY-10197R
    Wortmannin (Standard)
    		Inhibitor
    Wortmannin (Standard) is the analytical standard of Wortmannin. This product is intended for research and analytical applications. Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.
    Wortmannin (Standard)
  • HY-13715BR
    Norepinephrine bitartrate monohydrate (Standard)
    		Inducer
    Norepinephrine (bitartrate monohydrate) (Standard) is the analytical standard of Norepinephrine (bitartrate monohydrate). This product is intended for research and analytical applications. Norepinephrine (Levarterenol; L-Noradrenaline) bitartrate monohydrate is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
    Norepinephrine bitartrate monohydrate (Standard)
  • HY-Y1269H
    Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC
    		Inhibitor
    Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC (Salmiac, meets analytical specification of Ph. Eur. BP USP FCC) 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, meets analytical specification of Ph. Eur. BP USP FCC
  • HY-B1227S1
    Carprofen-13C,d3
    Carprofen-13C,d3 is the deuterium and 13C labeled Carprofen[1]. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively[2][3][4].
    Carprofen-<sup>13</sup>C,d<sub>3</sub>
  • HY-162866
    CXM102
    		Activator
    CXM102 is an autophagy activator. CXM102 can induce autophagy in aged BMSCs, leading to the rejuvenation of BMSCs and preferential differentiation into osteoblasts. CXM102 promotes the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. CXM102 can stimulate bone synthesis metabolism in middle-aged male mice, reduce bone marrow adipocytes, delay bone loss, lower serum inflammation levels, decrease organ fibrosis, and extend the lifespan of the mice.
    CXM102
  • HY-W584520
    Thalidomide-4-NH-PEG1-NH-Boc
    		Inducer
    Thalidomide-4-NH-PEG1-NH-Boc is a Boc-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-4-NH-PEG1-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-4-NH-PEG1-NH-Boc
  • HY-13955S1
    Telmisartan-d4
    		Inducer
    Telmisartan-d4 is the deuterium labeled Telmisartan. 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[1][2].
    Telmisartan-d<sub>4</sub>
  • HY-17504C
    (3R,5R)-Rosuvastatin
    		Activator
    (3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    (3R,5R)-Rosuvastatin
  • HY-10820S
    Pemetrexed-d5
    Pemetrexed-d5 is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[2].
    Pemetrexed-d<sub>5</sub>
  • HY-125535
    OSU-53
    		Inducer
    OSU-53 is an orally active AMPK activator (EC50: 0.3 μM) and a direct mTOR inhibitor. OSU-53 induces autophagy and increases conversion of LC3 I to LC3 II. OSU-53 also modulates energy homeostasis by suppressing fatty acid biosynthesis and shifting the metabolism to oxidation by up-regulating the expression of PGC1α and NRF-1. OSU-53 has antitumor activity in various tumor models, such as breast cancer and thyroid cancer.
    OSU-53
  • HY-147520
    FAK-IN-5
    		Inducer
    FAK-IN-5 (Compound 8l) is a FAK signaling inhibitor. FAK-IN-5 induces cell apoptosis and autophagy.
    FAK-IN-5
  • HY-12956S1
    Dinoprost-d9
    		Inducer
    Dinoprost-d9 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour[1][2].
    Dinoprost-d<sub>9</sub>
  • HY-50878AS
    Crizotinib-d9 hydrochloride
    		Inducer
    Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.
    Crizotinib-d<sub>9</sub> hydrochloride
  • HY-N0400R
    Wogonin (Standard)
    		Inducer
    Wogonin (Standard) is the analytical standard of Wogonin. This product is intended for research and analytical applications. Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
    Wogonin (Standard)
  • HY-B1030R
    Lanatoside C (Standard)
    		Inducer
    Lanatoside C (Standard) is the analytical standard of Lanatoside C. This product is intended for research and analytical applications. Lanatoside C is a cardiac glycoside, can be used in the treatment of congestive heart failure and cardiac arrhythmia.Lanatoside C has an IC50 of 0.19 μM for dengue virus infection in HuH-7 cells. Lanatoside C can effectively inhibit all four serotypes of dengue virus, flavivirus Kunjin, alphavirus Chikungunya, Sindbis virus and the human enterovirus 71.
    Lanatoside C (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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