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-10234R
    Saracatinib (Standard)
    		Inducer
    Saracatinib (Standard) is the analytical standard of Saracatinib. This product is intended for research and analytical applications. Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases[1].
    Saracatinib (Standard)
  • HY-12855
    Lys01
    		Inhibitor
    Lys01, a dimeric form of Chloroquine (HY-17589A), is an autophagy inhibitor. Lys01 inhibits cell viability of 1205Lu, c8161, LN229, HT-29 cells with IC50s of 3.6, 3.8, 7.9, 6.0 μM. Lys01 can be used for anticancer research.
    Lys01
  • HY-N13176
    Stellettin B
    		Inducer
    Stellettin B is a triterpenoid compound that can be isolated from the marine sponge Jaspis stellifera. Stellettin B induces G1 phase arrest, apoptosis, and autophagy in human non-small cell lung cancer A549 cells by blocking the PI3K/Akt/mTOR pathway. Stellettin B can reduce the migration and invasion of liver cancer cells by decreasing the activation of the MAPK and FAK/PI3K/AKT/mTOR signaling pathways. Stellettin B can be used in the study of various tumors.
    Stellettin B
  • HY-158117
    [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2
    		Inducer
    [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 (Compound 3) is a copper complex, which inhibits cell viability of HCT116, HCT116DoxR, A2780 and fibroblasts, with IC50s of 0.13, 0.15, 0.66 and 6.24 μM, respectively. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 induces apoptosis and autophagy, and arrests cell cycle at G0/G1 phase in HCT116DoxR. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 exhibits antimetastatic efficacy.
    [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2
  • HY-N0102R
    Isoliquiritigenin (Standard)
    		Inducer
    Isoliquiritigenin (Standard) is the analytical standard of Isoliquiritigenin. This product is intended for research and analytical applications. Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza uralensis Fisch., which inhibits aldose reductase with an IC50 of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC50 of 24.7 μM.
    Isoliquiritigenin (Standard)
  • HY-10255AR
    Sunitinib (Standard)
    		Inducer
    Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib (Standard)
  • HY-15388S2
    Tazarotene-13C6
    Tazarotene-13C6 (AGN 190168-13C6) is 13C labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Tazarotene-<sup>13</sup>C<sub>6</sub>
  • HY-111505A
    NAcM-OPT hydrochloride
    		Inducer
    NAcM-OPT (hydrochloride) is a protein interaction inhibitor. NAcM-OPT (hydrochloride) can disrupt the interaction between DCN1 and UBC12, with an IC50 value of 80 nM. NAcM-OPT (hydrochloride) can protect keratinocytes from H2O2-induced cell damage by promoting autophagy.
    NAcM-OPT hydrochloride
  • HY-50878R
    Crizotinib (Standard)
    		Inducer
    Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. 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 (Standard)
  • HY-101840AR
    EIPA hydrochloride (Standard)
    		Activator
    EIPA (hydrochloride) (Standard) is the analytical standard of EIPA (hydrochloride). This product is intended for research and analytical applications. EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma[1][2][3][5].
    EIPA hydrochloride (Standard)
  • HY-10260A
    Vandetanib trifluoroacetate
    		Inducer
    Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
    Vandetanib trifluoroacetate
  • HY-50898S4
    Lapatinib-d7
    		Inducer
    Lapatinib-d7 (GW572016-d7) 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.
    Lapatinib-d<sub>7</sub>
  • HY-14649S6
    Retinoic acid-d3-1
    Retinoic acid-d3-1 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
    Retinoic acid-d<sub>3</sub>-1
  • HY-10208R
    Pazopanib (Standard)
    		Inducer
    Pazopanib (Standard) is the analytical standard of Pazopanib. This product is intended for research and analytical applications. 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 (Standard)
  • HY-13417R
    AICAR (Standard)
    		Inhibitor
    AICAR (Standard) is the analytical standard of AICAR. This product is intended for research and analytical applications. AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
    AICAR (Standard)
  • HY-13749BR
    Sitagliptin (phosphate monohydrate) (Standard)
    		Inhibitor
    Sitagliptin (phosphate monohydrate) (Standard) is the analytical standard of Sitagliptin (phosphate monohydrate). This product is intended for research and analytical applications. Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    Sitagliptin (phosphate monohydrate) (Standard)
  • HY-10572S
    Efavirenz-d5
    		Inducer
    Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. Efavirenz-d5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Efavirenz-d<sub>5</sub>
  • HY-17464S2
    Cilostazol-d2
    		Inducer
    Cilostazol-d2 (OPC 13013-d2) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM.
    Cilostazol-d<sub>2</sub>
  • HY-122047
    SW063058
    SW063058 is an autophagy inducer that specifically disrupts the binding of Beclin 1 to Bcl-2 while leaving the interaction between Bcl-2 and pro-apoptotic members like Bax and BIM unaffected. By inhibiting the negative regulatory effects of Bcl-2 on Beclin 1, which is crucial for the initiation of autophagy, SW063058 promotes autophagic activity without triggering cytotoxicity, apoptosis, or other forms of cell death in vitro.
    SW063058
  • HY-10402R
    Losmapimod (Standard)
    		Inhibitor
    Losmapimod (Standard) is the analytical standard of Losmapimod. This product is intended for research and analytical applications. Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively[1].
    Losmapimod (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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