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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
2413 Results for "
paraoxon-induced cholinergic toxicity
" in MedChemExpress (MCE) Product Catalog:
Products (2413)
2413 Results for "paraoxon-induced cholinergic toxicity" in MCE Product Catalog:
YHO-13351 is an orally active ABCG2 inhibitor . YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer .
Cat. No.: HY-160062
S2.2 aptamer sodium is a nucleic acid-based MUC1-binding aptamer with high affinity and low toxicity. Upon binding to its target, S2.2 aptamer sodium undergoes a conformational switch and restores fluorescence signal, serving as a targeted imaging agent for MUC1-positive cancer cells. S2.2 aptamer sodium enables targeted delivery to breast cancer cells with overexpressed MUC1. When formulated as the S2.2-PEG-MZF molecular probe, S2.2 aptamer sodium possesses the functions of T2 signal inhibition, magnetic field-induced hyperthermia and targeted magnetic resonance molecular imaging. In the S2.2-PEG-MZF/DOX nanoliposome, S2.2 aptamer sodium supports targeted thermochemotherapy, effectively inhibiting cancer cell proliferation and invasion as well as inducing apoptosis, and is widely used in studies related to breast cancer .
Cat. No.: HY-161995
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells .
Cat. No.: HY-164288
CAS No.: 2287331-29-5
Synonyms: TDI-006570
Target:
Research Areas:
TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC50 of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases .
Cat. No.: HY-175236
CAS No.: 3053768-78-5
Research Areas:
SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research .
Cat. No.: HY-178032
Research Areas:
PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy .
Cat. No.: HY-182354
CAS No.: 861877-12-5
VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors .
Cat. No.: HY-182745
VEGFR-2-IN-85 is a strong VEGFR-2 inhibitor, with an IC50 value of 0.23 μM. VEGFR-2-IN-85 exhibits potent cytotoxic activity against multiple cancer cell lines with minimal toxicity toward normal cells. VEGFR-2-IN-85 also impairs cancer cell migration, likely through modulation of the VEGFR-2/p-Akt pathway. VEGFR-2-IN-85 can induce apoptosis through modulation of Caspase-3, Bax and Bcl-2. VEGFR-2-IN-85 arrests cell cycle at the G2/M phase and has anti-angiogenic activity. VEGFR-2-IN-85 is a targeted radiosensitizer enhancing radiation-induced cytotoxicity. VEGFR-2-IN-85 can be used for research on cancers such as non-small cell lung cancer, breast cancer, and liver cancer .
Cat. No.: HY-184158
Target:
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HATC is a HIF-1α AUTAC degrader. HATC links HIF-1α to LC3 to form a ternary complex that undergoes degradation via the autophagy-lysosome fusion pathway. HATC induces dose-dependent HIF-1α degradation in multiple cell types. HATC reduces visceral fat accumulation, hepatic lipid deposition, senescent cell aggregation, and bone loss; alleviates age-related intervertebral disc degeneration, liver dysfunction, kyphosis, and alveolar dilation; decreases circulating lactic acid levels; improves physical performance; and reverses age-related changes in granulocyte proportions. HATC extends median and maximum lifespan, reduces transcriptomic age, and causes no obvious persistent toxicity. HATC can be used in the research of age-related diseases (pink: LC3 ligand (HY-50759); blue: HIF-1α ligand (HY-P10426); Linker: (HY-W008264)) .
Cat. No.: HY-B0366AR
CAS No.: 969-33-5
Synonyms: Cyproheptadine HCl (Standard)
Target:
Reference Standards p38 MAPK Checkpoint Kinase (Chk) Histamine Receptor 5-HT Receptor CDK PARP Apoptosis
Research Areas:
Cyproheptadine hydrochloride (Standard) (Cyproheptadine HCl (Standard)) is the analytical standard of Cyproheptadine hydrochloride (HY-B0366A). This product is intended for research and analytical applications. Cyproheptadine hydrochloride (Cyproheptadine HCl) acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .
Target:
Reference Standards p38 MAPK Checkpoint Kinase (Chk) Histamine Receptor 5-HT Receptor CDK PARP Apoptosis
Research Areas:
Cyproheptadine (Standard) is the analytical standard of Cyproheptadine (HY-B1622). This product is intended for research and analytical applications. Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .
Cat. No.: HY-B1622S
CAS No.: 2712455-05-3
Target:
Isotope-Labeled Compounds p38 MAPK Checkpoint Kinase (Chk) Histamine Receptor 5-HT Receptor CDK PARP Apoptosis
Research Areas:
Cyproheptadine-d3 is the d3-labeled Cyproheptadine (HY-B1622). Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .
Cat. No.: HY-B1953R
CAS No.: 111988-49-9
Target:
Research Areas:
Thiacloprid (Standard) is the analytical standard of Thiacloprid. This product is intended for research and analytical applications. Thiacloprid is an orally active neurotoxic insecticide and also a nAChR agonist. Thiacloprid reduces the viability of healthy cells, depletes reduced glutathione, and increases MDA levels, thereby inducing cytotoxicity and oxidative stress damage. In practical applications, Thiacloprid has lower acute toxicity to honeybees than other compounds of the same class such as Imidacloprid (HY-B0838), but it still significantly impairs the learning and memory function, immune capacity and survival status of honeybees. Thiacloprid induces intestinal microbial dysbiosis and reduces survival rate in middle-aged honeybees, increases the risk of premature collapse in bumblebee colonies, and significantly decreases the final colony weight and reproductive output. Thiacloprid is used in broad-spectrum agricultural pest control, often alone or in combination with Deltamethrin (HY-B1971), and meets the pest management needs of various crops including potatoes, cabbages, various fruits and vegetables, and nuts .
Cat. No.: HY-W720629
CAS No.: 21420-37-1
Cat. No.: HY-W783351
CAS No.: 1416808-87-1
Synonyms: Coppersensor 790 acetoxymethyl ester
Target:
Research Areas:
CS790AM (Coppersensor 790 acetoxymethyl ester) is a cell-permeable, Cu +-targeted near-infrared fluorescent probe (λabs=760 nm, λem=790 nm) applicable to live cells. CS790AM can cross lipophilic cell membranes, and is converted into negatively charged CS790 under the action of intracellular esterases to be retained, thus enabling highly sensitive, reversible "turn-on" detection of labile Cu + pools in live cells and mice. CS790AM possesses excellent biocompatibility and selectivity, avoids interference from other metal ions, shows no obvious toxicity, and can be rapidly cleared. CS790AM allows long-term longitudinal monitoring of individual mice, visualizes copper levels in internal organs and isolated livers, and effectively evaluates abnormal copper accumulation in Wilson's disease models (Atp7b -/-) as well as dynamic changes after chelator treatment. CS790AM can be used for research on Wilson's disease and related copper metabolic disorders .
Cat. No.: HY-L941
4,236 compounds
Orthosteric sites are highly conserved, leading to poor subtype selectivity, off-target toxicity and drug resistance in traditional drugs. By contrast, allosteric sites show low conservation, high hydrophobicity, weak polarity, confined geometry and dynamic cryptic properties, granting modulators high selectivity, functional tunability and safety. Thus, allosteric therapy has become a major focus in drug discovery.
MCE curated nearly 1,000 clinical-stage allosteric modulators, analyzed PDB complex structures to identify key pharmacophores and privileged scaffolds, then designed and filtered compounds using rational “scaffold derivation + physicochemical screening” with strict property criteria. The resulting compounds show high rigidity and shape complementarity to shallow, dynamic, hydrophobic allosteric pockets.
This library comprises 4,315 diverse, lead-like compounds ideal for allosteric drug discovery and target screening, covering kinases, GPCRs and more. All are analogs of clinical-stage molecules with similarity > 0.6, combining high druggability and allosteric binding potential to support efficient early-stage R&D.
Cat. No.: HY-121337R
CAS No.: 61213-25-0
Synonyms: R-40244 (Standard)
Target:
Reference Standards Environmental Pollutants Apoptosis Bcl-2 Family Herbicide HSP PERK Eukaryotic Initiation Factor (eIF) Akt GSK-3 Reactive Oxygen Species (ROS)
Research Areas:
Flurochloridone (Standard) (R-40244 (Standard)) is the analytical standard of Flurochloridone (HY-121337). This product is intended for research and analytical applications. Flurochloridone (R-40244) is an orally active herbicide and an inducer of ER stress, apoptosis, and cytotoxicity. Flurochloridone upregulates GRP78 and activates the PERK-eIF2α-ATF4 UPR axis, ATF6, CHOP, Bax, and Bim. Flurochloridone decreases Akt, p-Akt, GSK3β, and p-GSK3β levels, and induces ROS, oxidative stress, γ-glutamyl cycle activation, and GSH accumulation. Flurochloridone inhibits mitochondrial respiration and ATP production while enhancing glycolysis and cell viability inhibition. Flurochloridone inhibits spermatogonial proliferation, spermatocyte meiosis, and sperm mitochondrial membrane potential, and induces Sertoli cell apoptosis and mitochondrial damage. Flurochloridone non-competitively binds phytoene desaturase, blocking phytoene desaturation and carotenoid synthesis, leading to leaf bleaching and phytotoxicity. Flurochloridone can be used for research on male reproductive toxicity, hepatotoxicity, and as a herbicide .
Cat. No.: HY-141878
CAS No.: 2767983-76-4
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Research Areas:
di-Ellipticine-RIBOTAC is a RNase recruiting chimera (RIBOTAC) degrader, capable of specifically binding and degrading expanded G4C2 RNA repeat (r(G4C2) exp). di-Ellipticine-RIBOTAC selectively binds the three-dimensional (3D) structure formed by r(G4C2) exp and that recruits an endogenous ribonuclease (RNase) to cleave r(G4C2) exp. di-Ellipticine-RIBOTAC selectively degrades the mutant chromosome 9 open reading frame 72 (C9orf72) allele and reduces quantities of toxic dipeptide repeat proteins (DPRs) translated from r(G4C2) exp. di-Ellipticine-RIBOTAC significantly improves the pathological phenotype of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) in cells and mouse models. di-Ellipticine-RIBOTAC can be used for the study of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) .
Cat. No.: HY-173033
CAS No.: 2530027-71-3
Research Areas:
MI-883 is orally active constitutive androstane receptor (CAR) (EC50 of 73 nM) agonist and pregnane X Receptor (PXR) (IC50 of 100 nM) antagonist. MI-883 binds to CAR and PXR ligand-binding domains, promotes CAR LBD assembly, activates CAR3 variant, stimulates CAR cytoplasmic-nuclear translocation, upregulates CAR target genes, recruits coactivators NCOA1, NCOA2, NCOA3, inhibits basal and agonist-induced PXR activation, downregulates PXR target genes, disrupts PXR-NCOR2 interaction, blocks agonist-mediated PXR-NCOA1 recruitment. MI-883 reduces plasma total cholesterol, LDL cholesterol, and hepatic free cholesterol levels, increases fecal bile acid excretion, regulates genes involved in xenobiotic metabolism, cholesterol homeostasis, and bile acid homeostasis. MI-883 exhibits metabolic stability, liver-predominant distribution, a safety profile with no observed toxicity, and does not stimulate human hepatocyte hypertrophy or hyperplasia. MI-883 can be used for the research of diet-induced hypercholesterolemia .
Cat. No.: HY-173148
CAS No.: 2892688-18-3
TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC50 of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC50 as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC50 of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
