Esophageal Cancer

ML385 is a potent and selective Nrf2 inhibitor with an IC₅₀ of 1.9 μM. ML385 directly binds to the Neh1 domain of NRF2, interferes with the binding of the MAFG-NRF2 protein complex to the antioxidant response element (ARE) DNA sequence, thereby blocking the expression of downstream target genes of NRF2. ML385 can be used in studies related to adult T-cell leukemia, breast cancer, myocardial ischemia/reperfusion injury, non-small cell lung cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and lung squamous cell carcinoma.

Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing Trastuzumab deruxtecan (HY-138298A) and Patritumab deruxtecan (HY-P99813).

BL-B01D1 (Izalontamab Brengitecan) is a bispecific antibody-drug conjugate (ADC) targeting EGFR and HER3, formed by conjugating the EGFR/HER3 bispecific antibody Izalontamab (HY-P99676) to a novel TOP-I inhibitor payload Deruxtecan 2-hydroxypropanamide (HY-153891) via a cleavable linker (Mc-Gly-Gly-Phe-Gly). BL-B01D1 binds to EGFR and HER3 on the surface of tumor cells, mediates endocytosis and releases the payload, inhibits topoisomerase I, blocks DNA replication and RNA synthesis, and disrupts DNA structure. BL-B01D1 induces cell cycle S-phase arrest, apoptosis, antibody-dependent cell-mediated cytotoxicity, and tumor cell death. BL-B01D1 can be used for cancer research.

NCT-501 is a reversible, non-competitive, selective, blood-brain barrier-permeable ALDH1A1 inhibitor with an IC₅₀ of 40 nM. NCT-501 inhibits the AKT-β-catenin signaling pathway, induces necroptosis in nasopharyngeal carcinoma cells, suppresses their proliferation and inhibits stem cell spheroid formation. NCT-501 can be used in research related to nasopharyngeal carcinoma, esophageal squamous cell carcinoma and malignant tumors.

KY386 is a DHX33 helicase inhibitor with an IC₅₀ of 0.019 μM. KY386 inhibits the cell viability of various cancer cells. KY386 induces ferroptosis in cancer cells, and induces apoptosis in some cancer cell lines. KY386 increases the intracellular levels of ROS, LPO and Fe²⁺, and decreases the level of GSH in cancer cells. KY386 inhibits the growth of gastric cancer and colon cancer xenografts in nude mice. KY386 is applicable to the related research on liver cancer, lung cancer, pancreatic cancer, colorectal cancer, gastric cancer, breast cancer, leukemia, renal cancer, prostate cancer, esophageal cancer, cervical cancer, brain cancer (glioblastoma) and melanoma.

4-trans-Hydroxycyclohexylamine (trans-4-Aminocyclohexan-1-ol) is an intermediate. 4-trans-Hydroxycyclohexylamine is used in the synthesis of the PGK1 inhibitor Compd 25-4. 4-trans-Hydroxycyclohexylamine is used in research on EGFR-positive esophageal squamous cell carcinoma.

Methylnissolin-3-O-glucoside is a flavonoid glycoside derivative of Methylnissolin (HY-N2484). Methylnissolin-3-O-glucoside is isolated from plants of the genus Astragalus (Leguminosae). Methylnissolin-3-O-glucoside effectively induces the expression of AKT/Nrf2 and its downstream target genes HO-1 and NQO1. Methylnissolin-3-O-glucoside inhibits TNF-α-induced phosphorylation of MEK and ERK. Methylnissolin-3-O-glucoside exhibits free radical scavenging activity. Methylnissolin-3-O-glucoside inhibits cell proliferation and cell migration. Methylnissolin-3-O-glucoside is used in research on esophageal squamous cell carcinoma.

LD-110 trihydrochloride is a PROTAC degrader targeting LSD1 with a DC₅₀ of 0.44-1.24 μM. LD-110 trihydrochloride acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 trihydrochloride induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 trihydrochloride inhibits tumor growth in the KYSE-150 xenograft model. LD-110 trihydrochloride can be used in research related to esophageal squamous cell carcinoma.

LD-110 is a PROTAC degrader targeting LSD1 with a DC₅₀ of 0.44-1.24 μM. LD-110 acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 inhibits tumor growth in the KYSE-150 xenograft model. LD-110 can be used in research related to esophageal squamous cell carcinoma.

Kumatakenin is an orally active apoptosis inducer and autophagy inhibitor, with a K_d value of 2.94 μM for mouse ATG5. Kumatakenin increases the activities of caspase-3, caspase-8 and caspase-9, thereby inducing caspase-dependent apoptosis in ovarian cancer cells. Kumatakenin reduces the expression of chemokines and pro-oncogenic factors in ovarian cancer cells, and inhibits M2 macrophage polarization. Kumatakenin inactivates TRIM65 function, reduces the expression and stability of FASN, and thus inhibits the proliferation, migration, invasion and tumor progression of esophageal cancer cells. Kumatakenin interacts with ATG5 to reduce its protein level, decrease LC3 level, and reduce the number of autophagosomes in the hippocampus. Kumatakenin binds to Eno3 to upregulate its expression, reduce the stability and expression level of IRP1 mRNA, inhibit ferroptosis, alleviate intestinal inflammation, and restore epithelial barrier function. Kumatakenin enhances the efficacy of antibiotics against pathogenic bacteria, inhibits SARS-CoV-2 replication, and reduces cytokine production. Kumatakenin is applicable to research related to ovarian cancer, esophageal cancer, depression and colitis.

SHP2-D26 is a SHP2 PROTAC degrader with DC₅₀ values of 6.0 nM (KYSE520 cells) and 2.6 nM (MV4;11 cells), respectively. SHP2-D26 inhibits ERK phosphorylation, upregulates Bim levels, downregulates Mcl-1 levels, and induces cell cycle arrest and apoptosis. SHP2-D26 can be used in studies related to esophageal cancer, acute myeloid leukemia and non-small cell lung cancer.

Fumonisin B2 is a selective ceramide synthase inhibitor and carcinogenic mycotoxin with toxicity comparable to that of Fumonisin B1 (HY-N6719). Fumonisin B2 inhibits de novo sphingolipid biosynthesis by blocking the amide bond formation between fatty acids and dihydrosphingosine, which leads to a massive intracellular accumulation of free dihydrosphingosine, altered sphingosine levels, subsequent inhibition of cell proliferation, and induction of cell death. Fumonisin B2 is used to investigate the pathogenesis of diseases associated with Fusarium verticillioides contamination, including equine leukoencephalomalacia, porcine pulmonary edema syndrome, human esophageal cancer, and rat hepatocellular carcinoma.

VVD 065 is an orally active KEAP1-dependent NRF2 molecular glue degrader with a KEAP1 K_D of 65 nM. VVD 065 covalently engages KEAP1 at Cys151, allosterically stabilizes KEAP1-CUL3 complex formation and enhances NRF2 polyubiquitination and proteasomal degradation. VVD 065 can be used for the research of esophageal squamous cell carcinoma, lung cancer, head-and-neck cancer, uterine cancers.

LD-110 triTFA is a PROTAC degrader targeting LSD1 with a DC₅₀ of 0.44-1.24 μM. LD-110 triTFA acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 triTFA induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 triTFA inhibits tumor growth in the KYSE-150 xenograft model. LD-110 triTFA can be used in research related to esophageal squamous cell carcinoma.

KBU2046 is an orally active transforming growth factor-β (TGF-β1) inhibitor. KBU2046 reduces integrin family protein expression, decreases Raf, RIPK1 and ERK phosphorylation to deactivate the ERK signaling pathway, and down-regulates genes linked to TGF-β1 maturation. KBU2046 suppresses tumor cell motility, impedes cancer invasion and metastasis, and inhibits human ESCC growth and metastasis in a murine model. KBU2046 can be used for the researches of triple-negative breast cancer and esophageal squamous cell carcinoma.

CQY684 (PCA062 antibody) is a monoclonal antibody targeting CDH3/P-cadherin, which locks P-cadherin in an X-dimer conformation and enhances the stability of this adhesion structure. CQY684 induces P-cadherin phosphorylation and promotes its dissociation from the cytoplasmic region of P-cadherin. As an endocytosis inducer and lysosome-targeting agent, CQY684 facilitates the internalization of the P-cadherin-CQY684 complex and improves the turnover efficiency of P-cadherin. CQY684 serves as a platform for the delivery of intracellular anticancer compounds, which is achieved through the targeted lysosomal transport of the antibody-P-cadherin complex. CQY684 is applicable to the research of breast cancer, esophageal cancer, and head and neck cancer.

Benzo[a]pyrene diol epoxide is a carcinogen present in tobacco smoke as well as in environmental pollution. Benzo[a]pyrene diol epoxide is a metabolite of benzo[a]pyrene (BaP) , which is polycyclic aromatic hydrocarbon (PAH) . Benzo[a]pyrene diol epoxide induces esophageal carcinogenesis. Benzo[a]pyrene diol epoxide may act to induce activation of ERKs and p38 MAPK marked by an increased level of phosphorylation of both the ERKs and p38 MAPK which corresponds with the increased activation of both kinases as evidenced by increased phsosphorylation of their substrates Elk-1 and ATF-2, respectively.

PROTAC KDM4 degrader-1 is a KDM4 PROTAC degrader that degrades KDM4A-C with DC₅₀ values of 37.53, 39.93, and 49.41 nM, respectively, while sparing KDM4D. PROTAC KDM4 degrader-1 induces cell cycle arrest, apoptosis and antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 can be used for the research of esophageal cancer.

LRPPRC-IN-1 is a LRPPRC inhibitor. LRPPRC-IN-1 exerts dual effects of inhibiting LRPPRC activity and inducing its degradation by binding to the RNA-binding domain of LRPPRC. LRPPRC-IN-1 downregulates the expression of mitochondrial OXPHOS complex subunits and ATP synthase, inhibits oxidative phosphorylation, reduces ATP production, suppresses the proliferation and colony formation of various cancer cells, and inhibits tumor growth in vivo. LRPPRC-IN-1 can be used in studies related to lung cancer, pancreatic cancer, breast cancer, esophageal cancer, colorectal cancer, lymphoma, melanoma, cervical cancer, ovarian cancer, and prostate cancer.

Atg4B-IN-3 (compound a25) is a ATG4B inhibitor with a K_d value of 18.01 nM against the human target. Atg4B-IN-3 stably regulates the closed conformation of the loop, prevents substrates from accessing the catalytic site Cys74, and thereby inhibits the proteolytic activity of ATG4B. Atg4B-IN-3 blocks autophagic flux, reduces LC3-II levels, promotes p62 accumulation, disrupts autophagy homeostasis and enhances cell death. Atg4B-IN-3 inhibits cell proliferation, migration and clonogenic survival capacity. Atg4B-IN-3 can be used in studies related to esophageal squamous cell carcinoma.