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-157497
    DA5-HTL
    		Inducer
    DA5-HTL is a compound combined dasatinib with HaloTag system efficiently inhibits the growth of the cancer cells with GI50 of 1.923 nM.
    DA5-HTL
  • HY-17507CS
    (R)-(+)-Pantoprazole-d6
    (R)-(+)-Pantoprazole-d6 is deuterium labeled (R)-(+)-Pantoprazole.
    (R)-(+)-Pantoprazole-d<sub>6</sub>
  • HY-16558R
    Butein (Standard)
    		Inducer
    Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
    Butein (Standard)
  • HY-50898S3
    Lapatinib-d4-1
    		Inducer
    Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
    Lapatinib-d<sub>4</sub>-1
  • HY-W013075R
    Rutin (trihydrate) (Standard)
    		Inhibitor
    Rutin (trihydrate) (Standard) is the analytical standard of Rutin (trihydrate). This product is intended for research and analytical applications. Rutin (Rutoside) trihydrate is a multifunctional natural flavonoid glycoside. Rutin trihydrate has been demonstrating excellent antioxidant, anti-inflammatory, anti-diabetic, and anti-carcinogenic properties. Cardioprotective and neuroprotective activities .
    Rutin (trihydrate) (Standard)
  • HY-N0824R
    Syringin (Standard)
    		Inhibitor
    Syringin (Standard) is the analytical standard of Syringin. This product is intended for research and analytical applications. Syringin (Eleutheroside B) is an active natural phenolic glycoside possessing various pharmacological activities, including anti-inflammatory, anti-irradiation, anti-osteoporosis and anticancer activities. Syringin also can be used to enhance memory, relieve fatigue, improve human cognition and protect ischemia heart against cerebrovascular damage, etc.
    Syringin (Standard)
  • HY-B0365AS
    Memantine-d6 hydrochloride
    		Inducer ≥98.0%
    Memantine-d6 (hydrochloride) is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].
    Memantine-d<sub>6</sub> hydrochloride
  • HY-141013
    Thalidomide-O-amido-PEG4-propargyl
    		Inducer
    Thalidomide-O-amido-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Thalidomide-O-amido-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-O-amido-PEG4-propargyl
  • HY-110189S1
    Pregnenolone monosulfate-d4 sodium
    		Inducer
    Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
    Pregnenolone monosulfate-d<sub>4</sub> sodium
  • HY-172204
    SIRT-IN-7
    		Inducer
    SIRT-IN-7 (Compound 7ba) is a SIRT inhibitor. SIRT-IN-7 can inhibit the expression of SIRT1, SIRT2, and SIRT3, and increase the acetylation and activation of p53. SIRT-IN-7 can inhibit the proliferation, and induce apoptosis and autophagy of breast cancer cells. SIRT-IN-7 has anti-tumor activity.
    SIRT-IN-7
  • HY-156164
    Thalidomide-5-NH-PEG2-NH2 hydrochloride
    		Inducer
    Thalidomide-5-NH-PEG2-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG2-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-5-NH-PEG2-NH2 hydrochloride
  • HY-151503
    MPM-1
    		Modulator
    MPM-1, a marine Eusynstyelamides mimic, is a potent anticancer agent. MPM-1 can rapidly kill cancer cells in vitro by inducing a necrosis-like death. MPM-1 has the ability to induce immunogenic cell death. MPM-1 causes perturbation of autophagy and lysosomal swelling in cancer cells.
    MPM-1
  • HY-157758
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3
    		Inducer
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker . (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3
  • HY-17507S
    Pantoprazole-d6
    		Inhibitor
    Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
    Pantoprazole-d<sub>6</sub>
  • HY-101714R
    Oxyphenisatin acetate (Standard)
    		Inducer
    Oxyphenisatin acetate (Standard) is the analytical standard of Oxyphenisatin acetate. This product is intended for research and analytical applications. Oxyphenisatin acetate, the pro-agent of oxyphenisatin, is used to be a laxative.
    Oxyphenisatin acetate (Standard)
  • HY-162910
    HDAC-IN-79
    		Inducer
    HDAC-IN-79 (compound 4) is an orally active dual xanthine oxidase-HDAC inhibitor (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM;), with significant in vivo anti-hyperuricemia and anti-tumor activities. HDAC-IN-79 is the most potent cell growth inhibitor (IC50=0.706 μM) of leukemia HL60 cells, induces apoptosis and autophagy, and can regulate the expression levels of signature biomarkers associated with intracellular HDAC inhibition.
    HDAC-IN-79
  • HY-136162A
    Thalidomide-4-O-C2-NH2
    		Inducer
    Thalidomide-4-O-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-4-O-C2-NH2
  • HY-13749C
    (S)-Sitagliptin phosphate
    		Inhibitor
    (S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (S)-Sitagliptin phosphate
  • HY-123597
    NSC 109555
    		Inducer
    NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
    NSC 109555
  • HY-16397AS
    Phenformin-d5 hydrochloride
    		Inhibitor
    Phenformin-d5 (hydrochloride) is the deuterium labeled Phenformin hydrochloride. Phenformin hydrochloride is an anti-diabetic agent from the biguanide class, can activate AMPK activity[1][2].
    Phenformin-d<sub>5</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
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