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-101349
    L 741742
    		Inducer 99.28%
    L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma.
    L 741742
  • HY-B0113S3
    Omeprazole-13C,d3
    		98.00%
    Omeprazole-13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868) is an orally active H+,K+-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole aslo has neuroprotective and antibacterial effects.
    Omeprazole-<sup>13</sup>C,d<sub>3</sub>
  • HY-148598
    Curcumin 5-8
    		Inducer 98.58%
    Curcumin 5-8 (CUR5-8) is a potent and orally active naturally active curcumin (CUR) analog. Curcumin 5-8 inhibits lipid droplet formation. Curcumin 5-8 increases autophagy and inhibits Apoptosis. Curcumin 5-8 improves insulin resistance and insulin sensitivity.
    Curcumin 5-8
  • HY-122232
    SW083688
    		Inhibitor 99.78%
    SW083688 is a selective TAOK2 inhibitor with an IC50 of 1.3 μM. SW083688 increases the abundance of p62 protein, inhibits autophagosome maturation, and blocks Autophagic flux. SW083688 is applicable for the research of non-small cell lung cancer and pancreatic cancer.
    SW083688
  • HY-132971
    Thalidomide-piperazine hydrochloride
    		Inducer 98.27%
    Thalidomide-piperazine hydrochloride is a synthetic E3 ligase ligand-linker conjugate, comprising a cereblon ligand based on Thalidomide (HY-14658) and one linker. Thalidomide-piperazine hydrochloride can be used in studies related to PROTAC synthesis.
    Thalidomide-piperazine hydrochloride
  • HY-105037A
    Forigerimod TFA
    		Inhibitor 99.88%
    Forigerimod TFA (IPP-201101 TFA) is a CD4 T-cell modulator. Forigerimod TFA is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod TFA can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
    Forigerimod TFA
  • HY-N0413
    Hupehenine
    		Inducer 99.0%
    Hupehenine is an orally active isosteroidal alkaloid that can be extracted from F. hupehensis. Hupehenine exhibits activities such as antitussive, expectorant, anticancer, and antiparasitic. In vitro, Hupehenine can also inhibit α-synuclein seeded fibril formation, making it applicable for the research of Parkinson's disease and other related disorders.
    Hupehenine
  • HY-10261R
    Afatinib (Standard)
    		Inducer
    Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib (Standard)
  • HY-W007355S1
    Skatole-d8
    		98.50%
    Skatole-d8 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38.
    Skatole-d<sub>8</sub>
  • HY-50878S
    Crizotinib-d5
    		Inducer 99.60%
    Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
    Crizotinib-d<sub>5</sub>
  • HY-143466
    ULK1-IN-2
    		Inhibitor 98.34%
    ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer).
    ULK1-IN-2
  • HY-B0483
    Tioxolone
    		Inducer 98.24%
    Tioxolone is an inhibitor for the carbonic anhydrase. Tioxolone exhibits anti-leishmanial, antitumor, and anti-inflammatory activities. Tioxolone can be used in research of acne and psoriasis.
    Tioxolone
  • HY-N0156S
    Oleanolic acid-d3
    		98.78%
    Oleanolic acid-d3 is the deuterium labeled Oleanolic Acid. Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.
    Oleanolic acid-d<sub>3</sub>
  • HY-14664AS
    Fluvastatin-d6 sodium
    		98.06%
    Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
    Fluvastatin-d<sub>6</sub> sodium
  • HY-N0733S4
    Glucosamine-15N hydrochloride
    		99%
    Glucosamine-15N (hydrochloride) is the 15N labeled Glucosamine hydrochloride. Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a
    Glucosamine-<sup>15</sup>N hydrochloride
  • HY-B1773AS
    Sodium propionate-13C
    		Activator 99.6%
    Sodium propionate-13C is the 13C labeled Propionate sodium (HY-B1773A). Sodium propionate is an orally active short-chain fatty acid. Sodium propionate can be produced by intestinal bacteria from the metabolism of dietary fiber. Sodium propionate increases PPAR-γ, inhibits NF-κB activation, and reduces COX-2 expression and NO production. Sodium propionate also induces Apoptosis and Autophagy. Sodium propionate reduces HSV-1-induced keratitis. Sodium propionate has anticancer effects against glioblastoma. Sodium propionate exhibits neuroprotective, antioxidant, and anti-inflammatory activities. Sodium propionate can be used in the research of spinal cord injury and Alzheimer's disease.
    Sodium propionate-<sup>13</sup>C
  • HY-10201S2
    Sorafenib-13C,d3
    		Inducer 98.35%
    Sorafenib-13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib-<sup>13</sup>C,d<sub>3</sub>
  • HY-144636
    Atg4B-IN-2
    		Inhibitor 98.03%
    Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition.
    Atg4B-IN-2
  • HY-152100
    CUR5g
    		Inhibitor 98.69%
    CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo.
    CUR5g
  • HY-10862
    FAAH inhibitor 1
    		98.30%
    FAAH inhibitor 1 (compound 3) is a selective reversible FAAH inhibitor. FAAH inhibitor 1 has no off-target activity with respect to other serine hydrolases. FAAH inhibitor 1 is exclusively specific against FAAH in rat brain with an IC50 value of 18 nM and had no missing protein bands in all the other tissues. FAAH inhibitor 1 can be used for neurological disorders research.
    FAAH inhibitor 1
Cat. No. Product Name / Synonyms Application Reactivity
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