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-10882S1
    Clotrimazole-d10
    		Inhibitor
    Clotrimazole-d10 is deuterated labeled Clotrimazole (HY-10882). Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.
    Clotrimazole-d<sub>10</sub>
  • HY-155785
    MTP
    		Inducer
    MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma.
    MTP
  • HY-161200
    Thalidomide-piperazine-C-azetidine-C2-OH
    		Inducer
    Thalidomide-piperazine-C-azetidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperazine-C-azetidine-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperazine-C-azetidine-C2-OH
  • HY-155182
    HDAC-IN-62
    		Inducer
    HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC50s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mouse brain.
    HDAC-IN-62
  • HY-N0168S
    Hesperetin-d3
    Hesperetin-d3 is the deuterium labeled Hesperetin[1]. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin regulates apoptosis[2][3].
    Hesperetin-d<sub>3</sub>
  • HY-17464S1
    Cilostazol-d4
    		Inducer
    Cilostazol-d4 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[1][2].
    Cilostazol-d<sub>4</sub>
  • HY-N0410R
    Daucosterol (Standard)
    		Inducer
    Daucosterol (Standard) is the analytical standard of Daucosterol. This product is intended for research and analytical applications. Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway.
    Daucosterol (Standard)
  • HY-N6939R
    Pseudolaric Acid B (Standard)
    		Inducer
    Pseudolaric Acid B (Standard) is the analytical standard of Pseudolaric Acid B. This product is intended for research and analytical applications. Pseudolaric Acid B is an orally active diterpene acid. Pseudolaric Acid B has anti-fungal, anti-fertility, anti-angiogenesis and anticancer activity, and can induce tumor cell apoptosis and autophagy. In addition, Pseudolaric Acid B can inhibit the secretion of hepatitis B virus (HBV) and has immunosuppressive effect, selectively inhibiting the proliferation of T lymphocytes and the production of IL-2.
    Pseudolaric Acid B (Standard)
  • HY-15025AS
    Sildenafil citrate-d8
    Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate[1]. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
    Sildenafil citrate-d<sub>8</sub>
  • HY-130965B
    Thalidomide-PEG3-NH2 hydrochloride
    		Inducer 98.02%
    Thalidomide-PEG3-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-PEG3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-PEG3-NH2 hydrochloride
  • HY-123237
    KRC-108
    		Inducer
    KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice.
    KRC-108
  • HY-B1490AS1
    Imipramine-d4
    		Inducer
    Imipramine-d4 is deuterium labeled Imipramine. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5][6].
    Imipramine-d<sub>4</sub>
  • HY-107811A
    Harmol hydrochloride
    		Inducer
    Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol hydrochloride can induce cell mitosis, Autophagy and Apoptosis. Harmol hydrochloride promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol hydrochloride has anti-tumor, anti-depressant and anti-aging activities. Harmol hydrochloride improves motor impairment in a mouse Parkinson's disease model.
    Harmol hydrochloride
  • HY-14595R
    Biochanin A (Standard)
    Biochanin A (Standard) is the analytical standard of Biochanin A. This product is intended for research and analytical applications. Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
    Biochanin A (Standard)
  • HY-17356S1
    Fenofibrate-d4
    Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
    Fenofibrate-d<sub>4</sub>
  • HY-B0006S
    Carvedilol-d3
    		Inducer
    Carvedilol-d3 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
    Carvedilol-d<sub>3</sub>
  • HY-143658
    SH498
    SH498, a novel Bmi-1-mediated antitumor agent, shows potent antiproliferative activity.
    SH498
  • HY-135564
    RK-682 hemicalcium
    		Inhibitor
    RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 hemicalcium inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24[2].
    RK-682 hemicalcium
  • HY-B0151S1
    Pregnenolone-13C2,d2
    Pregnenolone-13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[1][2][3][4].
    Pregnenolone-<sup>13</sup>C<sub>2</sub>,d<sub>2</sub>
  • HY-P0018R
    Pepstatin (Standard)
    		Inhibitor
    Pepstatin (Standard) is the analytical standard of Pepstatin. This product is intended for research and analytical applications. Pepstatin (Pepstatin A) is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin also inhibits HIV protease[1][2].
    Pepstatin (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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