esophageal

CAN508 is a potent ATP-competitive CDK9 cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9 cyclin T over other CDK cyclin complexes. [Antitumor activity.]

Pegamotecan (PEG-camptothecin) is a topoisomerase I (TOP1) inhibitor with anticancer activity, and it is used in the treatment of esophageal, non-small cell lung and pancreatic cancers.

Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy.

Carbenoxolone disodium (Duogastrone) salt is an agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise, the drug is low in toxicity.

Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.

Isobutyl decanoate (Decanoic acid isobutyl ester) can be used as a biomarker for esophageal squamous cell carcinoma and lung cancer, and can be isolated from wine.

Oxethazaine (Oxetacaine), a topical anesthetic, is used to prevent acid-induced esophageal pain.

PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).

Isorhamnetin (3-methylquercetin) is the methylated metabolite of quercetin. Quercetin is an important dietary flavonoid with in vitro antioxidant activity. Isorhamnetin prevents endothelial cell injuries from oxidized LDL via inhibition of lectin-like ox-LDL receptor-1 upregulation, interference of ox-LDL-mediated intracellular signaling pathway (p38MAPK activation, NF-kappaB nuclear translocation, eNOS expression) and the antioxidant activity of isorhamnetin. Isorhamnetin prevents endothelial dysfunction, superoxide production, and overexpression of p47phox induced by angiotensin II. Isorhamnetin appears to be a potent drug against esophageal cancer due to it's in vitro potential to not only inhibit proliferation but also induce apoptosis of Eca-109 cells.

Canertinib (CI-1033) is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.

QX 314 (Lidocaine N-ethyl bromide) is a blocker of non-membrane-permeable,and Inhibits Acid-Induced Activation of Esophageal Nociceptive C Fiber Neurons.

IV-23, a potent inhibitor of cell growth both in vitro and in vivo, effectively reduces colony formation, arrests the cell cycle at the M phase, and induces apoptosis in esophageal squamous cell carcinoma through Noxa-mediated pathways. This compound emerges as a promising anticancer agent with significant potential.

Lysipressin ([Lys8]-Vasopressin), Induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase. Lysipressin is Antidiuretic hormone that have been found in pigs and some marsupial families.

Itopride HCl is an AChE inhibitor and dopamine D2 receptor antagonist. It inhibits lower esophageal sphincter relaxation. It also used to treat functional dyspepsia and gastroesophageal reflux disease

Lobaplatin (D-19466) (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin (D-19466) is a third-generation platinum anti-neoplastic agent which shows activity for a variety of tumour types and is a promising antitumour chemotherapeutic agent[1][2]. It is a platinum complex with DNA alkylating activity.

CHI-KAT8i5 is a selective inhibitor of KAT8 with a KD of 19.72 μM. It induces apoptosis (Apoptosis) in a dose-dependent manner. CHI-KAT8i5 can inhibit tumor growth in esophageal squamous cell carcinoma, colon cancer, melanoma, gastric cancer, non-small cell adenocarcinoma, and liver cancer.

ZSH-2208, an analogue of retinoic acid A, exerts strong anti-tumor effects on regenerative stem cells (TRCs) in esophageal squamous cell carcinoma (ESCC) via the RARγ-TNFAIP3 pathway.

Monoethanolamine Oleate (Etamolin, FO-611) is a hardening agent used in the treatment of varicose and esophageal veins.

Sintilimab (IBI308) is a humanized IgG4 monoclonal antibody with significant anti-tumor activity that restores endogenous anti-tumor T-cell responses by binding to PD-1 and thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2).Sintilimab is used in combination with other compounds for the treatment of classical Hodgkin's lymphoma, non-cellular lung cancer and esophageal cancer. Sintilimab is used in combination with other compounds to treat classical Hodgkin's lymphoma, non-small cell lung cancer and esophageal cancer.

Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mammary carcinoma cells in a chamber cell migration assay (IC50= 29 μM).2It enhances cytotoxicity induced by vinblastine in vincristine-resistant P388/VCR cells.3

CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). SIRT3 is involved in modulating metabolic homeostasis as a NAD+-dependent protein deacetylase in the mitochondria. SIRT3 functions as either an oncogene or tumor suppressor, depending on cancer cell type. High SIRT3 expression in patient-derived esophageal cancer tissues is associated with shorter survival and, in mice, downregulation leads to a lower tumor load. In contrast, low SIRT3 expression in patient-derived breast cancer cells is correlated with shorter survival.

(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanothione reductase when used at a concentration of 200 μM.3(E)-Ajoene (25 mg/kg) is neuroprotective in a gerbil model of ischemia-reperfusion injury, reducing reactive astrocytosis and microgliosis in the hippocampal CA1 region.4 1.Yoshida, H., Iwata, N., Katsuzaki, H., et al.Antimicrobial activity of a compound isolated from an oil-macerated garlic extractBiosci. Biotechnol. Biochem.62(5)1014-1017(1998) 2.Kaschula, C.H., Hunter, R., Hassan, H.T., et al.Anti-proliferation activity of synthetic ajoene analogues on cancer cell-linesAnticancer Agents Med. Chem.11(3)260-266(2011) 3.Gallwitz, H., Bonse, S., Martinez-Cruz, A., et al.Ajoene is an inhibitor and subversive substrate of human glutathione reductase and Trypanosoma cruzi trypanothione reductase: Crystallographic, kinetic, and spectroscopic studiesJ. Med. Chem.42(3)364-372(1999) 4.Yoo, D.Y., Kim, W., Nam, S.M., et al.Neuroprotective effects of Z-ajoene, an organosulfur compound derived from oil-macerated garlic, in the gerbil hippocampal CA1 region after transient forebrain ischemiaFood Chem. Toxicol.721-7(2014)

N'-Nitrosonornicotine is a tobacco-specific N-nitrosamine and carcinogen that has been found in unburned tobacco and cigarette smoke.1It induces the formation of DNA adducts in isolated rat nasal mucosa and esophagus. N'-Nitrosonornicotine induces tumor formation in rat esophagus and nasal cavity, mouse lung, forestomach, and trachea, and hamster trachea and forebrain. Urinary levels of N'-nitrosonornicotine are positively correlated with the risk of esophageal cancer in smokers.2 1.Hecht, S.S.Biochemistry, biology, and carcinogenicity of tobacco-specific N-nitrosaminesChem. Res. Toxicol.11(6)559-603(1998) 2.Yuan, J.-M., Knezevich, A.D., Wang, R., et al.Urinary levels of the tobacco-specific carcinogen N'-nitrosonornicotine and its glucuronide are strongly associated with esophageal cancer risk in smokersCarcinogenesis32(9)1366-1371(2011)

Sucrose octasulfate (SOS), a component of the gastrointestinal protectant sucralfate, is an alkaline aluminum-sucrose complex that inhibits peptic hydrolysis and raises gastric pH, protecting esophageal epithelium against acid injury. It can bind to exosite II of thrombin (KD = ~1.4 μM) and inhibit its catalytic activity (IC50 = 4.5 μM) and, as such, has been used as a surrogate for heparin. Furthermore, SOS has been shown to inhibit tumor growth in mouse melanoma and lung carcinoma models by preventing fibroblast growth factor 2 (FGF-2) binding to endothelial cells and also by removing any pre-bound FGF-2 from these cells (IC50 = ~2 μg/ml).