Autophagy Inhibitor

Nortriptyline (Desmethylamitriptyline) hydrochloride, the main active metabolite of Amitriptyline, is a tricyclic antidepressant. Nortriptyline hydrochloride is a potent autophagy inhibitor and has anticancer effects.

IGF2BP1-IN-1, a Cucurbitacin B (HY-N0416) derivative, is a potent IGF2BP1 inhibitor (K_D = 2.88 nM). IGF2BP1-IN-1 binds directly to IGF2BP1, thereby inducing tumor cell cycle arrest, increasing apoptosis, and reducing autophagy. IGF2BP1-IN-1 can be used in research on NSLSC, colon, breast, liver, ovarian, pancreatic, and cervical cancers.

ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.

CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.

Isosorbide mononitrate (Isosorbide-5-mononitrate) is an orally active nitric acid compound used for angina pectoris by dilating blood vessels and lowering blood pressure. Isosorbide mononitrate increases the viability and proliferation of HUVECs by decreasing Apoptosis and elevated the expressions of vedf, kdrl, pdgfr in zebrafish embryos. Isosorbide mononitrate is promising for research of heart failure and coronary heart disease.

Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀ of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC₅₀=155 nM).

Gypenoside XLIX is a multifunctional bioactive compound that can be isolated from Gynostemma pentaphyllum, with a K_a value of 1.58 μM for its binding to SIRT1. Gypenoside XLIX acts as a PPAR-α agonist. It inhibits the activation of TLR4-mediated NF-κB signaling pathway by activating the Sirt1/Nrf2 signaling pathway, reduces ROS accumulation, and alleviates hepatic inflammatory injury in mice with sepsis-induced liver disease. Gypenoside XLIX targets SIRT1 to block YAP-NLRP3 activation and improve sepsis-induced cardiomyopathy. Gypenoside XLIX inhibits apoptosis (Apoptosis), pyroptosis (Pyroptosis), autophagy (Autophagy), lipid peroxidation, pro-inflammatory cytokines and anti-inflammatory cytokines. Gypenoside XLIX alleviates sepsis-induced splenic injury by inhibiting inflammation and oxidative stress, and mitigates sepsis-associated encephalopathy by targeting PPAR-α. Gypenoside XLIX prevents acute kidney injury by inhibiting IGFBP7/IGF1R-mediated programmed cell death and inflammation. Gypenoside XLIX inhibits the expression and activity of vascular cell adhesion molecule-1 in cytokine-induced human endothelial cells. Gypenoside XLIX is applicable to research related to acute liver injury, lung injury, cardiomyopathy, acute splenic injury, sepsis-associated encephalopathy, acute kidney injury, atherosclerosis and chronic inflammation.

Ganglioside GM1 is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease.

Oleanonic acid (3-Oxooleanolic acid) is an orally available triterpene that has anti-inflammatory and insecticidal properties. In vitro, oleanonic acid can improve oxidative stress, autophagy defects, ferroptosis, mitochondrial damage, and endoplasmic reticulum stress induced by Amyloid-β, and in vivo, it can alleviate myocardial hypertrophy in rats.

PDRN (Polydeoxyribonucleotide) is a deoxynucleotide polymer mainly derived from the sperm of rainbow trout or salmon. PDRN inhibits pro-inflammatory factors and promotes VEGF expression via the cAMP-PKA pathway by activating the adenosine A_2A receptor (A_2AR), thereby driving angiogenesis and collagen deposition in fibroblasts. Degradation products of PDRN provide DNA raw materials for proliferating cells through the salvage synthesis pathway, accelerating re-epithelialization. PDRN reduces melanin synthesis and cell apoptosis by upregulating ERK/AKT phosphorylation and inhibiting the activities of MITF and tyrosinase, and resists skin aging by attenuating nuclear autophagy and blocking the interaction between LC3-SIRT1. PDRN is mainly used for wound repair, post-aesthetic surgery recovery and anti-aging research.

THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC₅₀ of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.

SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC₅₀s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research.

MitoTEMPOL is a mitochondria-targeted superoxide scavenger. MitoTEMPOL accumulates in mitochondria via membrane potential and locally scavenges superoxide anions. MitoTEMPOL alleviates hepatic oxidative stress and alterations in genes related to autophagy in STZ (HY-13753)-induced diabetic models. MitoTEMPOL inhibits diaphragmatic mitochondrial dysfunction and activation of proteolytic pathways in sepsis models. MitoTEMPOL also alleviates AGEs (HY-NP165)-induced ferritinophagy-dependent ferroptosis in human umbilical vein endothelial cells. MitoTEMPOL is used in research related to diabetes, sepsis, and vascular endothelial ferroptosis.

Acetyl-coenzyme A (Acetyl-CoA) lithium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A lithium, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A lithium is also a key precursor of lipid synthesis.

ATG7-IN-1 (Compound 37) is a potent and selective inhibitor of ATG7 (IC₅₀ = 62 nM).

Pepstatin (Pepstatin A) Ammonium 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 Ammonium also inhibits HIV protease.

Methylprednisolone (Standard) is the analytical standard of Methylprednisolone. This product is intended for research and analytical applications. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.

PIK5-12d is a PROTAC PIKfyve degrader (DC₅₀ = 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d significantly suppresses tumor proliferation in mice bearing LTL-331R human prostate cancer PDX tumors. PIK5-12d can be used for the study of prostate cancer.

Recombinant humanized type III collagen (MW 55900) is a type III collagen with a molecular weight of 55900 Da. Recombinant humanized type III collagen has various biological functions, such as promoting skin extracellular matrix regeneration and improving the cell microenvironment. Recombinant humanized type III collagen inhibits the proliferation, migration, and invasion of breast cancer cells. Type III collagen functions in cell adhesion, migration, proliferation and differentiation through its interaction with integrins.

Melatonin-d₃ is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.