esophageal

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.

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.]

Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively.

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.

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.

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.

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

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 is a retinoic acid A analogue that inhibits tumour cell proliferation and survival through RARγ-TNFAIP3 and retinoid receptors.

(R)-(+)-Pantoprazole ((R)-(+)-BY1023) sodium is a proton pump inhibitor used in the study of esophageal erosion and ulcers.

PROTACKDM4 degrader-1 (Compound 11) is a proteolysis-targeting chimera (PROTAC) degrader specifically designed for KDM4. It effectively degrades KDM4A-C while sparing KDM4D. In esophageal cancer cells, PROTACKDM4 degrader-1 demonstrates strong antiproliferative activity, inducing apoptosis and cell cycle arrest, and inhibits lysine demethylation of histone H3.

P-gp inhibitor 29 (41) is a potent inhibitor of P-gp and an apoptosis inducer, with an IC50 value of 8.9 nM in Eca109/VCR cells, making it useful for esophageal cancer research.

HDAC/PSMD14-IN-1 is a derivative of gambogic acid. It serves as an orally active dual inhibitor targeting PSMD14 and HDAC1, with IC50 values of 238.7 nM and 141.2 nM, respectively. The compound exhibits significant cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). Additionally, HDAC/PSMD14-IN-1 can induce apoptosis. In KYSE30 cell xenograft models in mice, it displays antitumor activity. HDAC/PSMD14-IN-1 is useful for researching esophageal cancer treatment.

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.

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