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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
3492 Results for "
Competitive
" in MedChemExpress (MCE) Product Catalog:
Products (3492)
3492 Results for "Competitive" in MCE Product Catalog:
Synonyms: MK-678; L-363586
Target:
Cat. No.: HY-113416AS
Purity: 98.00%
Synonyms: DHEA sulfate-d6 sodium dihydrate; Prasterone sulfate-d6 sodium dihydrate
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DpC is a selective, orally active iron chelator with anticancer activity. DpC acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer .
Cat. No.: HY-114243A
CAS No.: 1382469-40-0
Target:
Research Areas:
Neurological Disease Inflammation/Immunology Endocrinology Cancer
DpC hydrochloride is a selective, orally active iron chelator with anticancer activity. DpC hydrochloride acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC hydrochloride induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC hydrochloride inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC hydrochloride is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer .
Cat. No.: HY-114849R
CAS No.: 27314-13-2
Synonyms: SAN 9789 (Standard)
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Norflurazon (Standard) (SAN 9789 (Standard)) is the analytical standard of Norflurazon (HY-114849). This product is intended for research and analytical applications. Norflurazon (SAN 9789) is a pre-emergence Herbicide. Norflurazon non-competitively inhibits phytoene desaturase by competing with the enzyme cofactor and disrupts carotenoid biosynthesis, thereby leading to chlorophyll photodegradation and chlorosis. Norflurazon inhibits MGDG synthase, CDP-choline phosphotransferase, Omega-3 FAD7 desaturase, and PG delta-3-trans desaturase, and activates LysoPC-acyltransferase and Omega-3 FAD3 desaturase. Norflurazon inhibits photosynthetic membrane organization, mitochondrial respiration, ATP production, PI3K signaling, and ERK1/2 phosphorylation. Norflurazon activates MAPK P38 phosphorylation and ER stress signaling. Norflurazon induces morphological malformations and cardiovascular effects in zebrafish embryos .
Cat. No.: HY-123597
CAS No.: 15427-93-7
Synonyms: DDUG; NCI C04808
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NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
Cat. No.: HY-178057
CAS No.: 2754394-10-8
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EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .
Cat. No.: HY-183393
CAS No.: 1798292-13-3
NVP-BHS345 is an ATP-competitive TORC1/TORC2 inhibitor with an IC50 of 1 μM for both targets in yeast. NVP-BHS345 acutely inhibits TORC1/TORC2 kinase activity, even in genetically engineered TOR1 M2282T Saccharomyces cerevisiae strains. NVP-BHS345 also reduces the phosphorylation levels of Ser-232/Ser-233 sites in Sch9, Ypk1/Ypk2 and Rps6, and induces hyperphosphorylation of Slt2 and activation of the cell wall integrity pathway. NVP-BHS345 causes depolarization of the actin cytoskeleton, blocks fluid-phase endocytosis, prevents the accumulation of vacuolar lipophilic dyes, and regulates the phosphorylation levels of Ent1, Pan1, Prk1, Akl1 and other cellular proteins .
Target:
TRP Channel Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Keap1-Nrf2 Amyloid-β Fungal Apoptosis
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Dyclonine (Dyclocaine) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
Cat. No.: HY-187361
CAS No.: 3107740-33-7
PROTAC HIV-1 degrader-1 is a HIV-1 capsid (CA) PROTAC degrader, with a DC50 of 3 nM against HIV-1IIIB (MT‑4 cells) and a DC50 of 1.17 nM against HIV-1NL4-3 (MT‑4 cells). PROTAC HIV-1 degrader-1 conjugates HIV-1 capsid (CA) with the VHL E3 ubiquitin ligase, triggering polyubiquitination and proteasome-mediated degradation of CA, as well as competitively inhibiting the binding of host factors CPSF6 and Sec24C to CA. PROTAC HIV-1 degrader-1 degrades CA drug-resistant mutants (N74D, K70R). PROTAC HIV-1 degrader-1 is applicable to research related to HIV-1 infection .
Cat. No.: HY-B0113S1
CAS No.: 934293-92-2
Synonyms: H 16868-d3-1
Cat. No.: HY-N0806R
CAS No.: 14215-86-2
Cat. No.: HY-N1957R
CAS No.: 31271-07-5
Synonyms: γ-Mangostin (Standard)
Cat. No.: HY-101140AR
CAS No.: 1799974-69-8
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KI696 isomer (Standard) is the analytical standard of KI696 isomer (HY-101140A). This product is intended for research and analytical applications. KI696 isomer is an isomer of KI696 (HY-101140). KI696 is a selective KEAP1/NRF2 protein-protein interaction inhibitor with a human Kd value of 1.3 nM. KI696 acts by competitively occupying the NRF2-binding pocket of the KEAP1 Kelch domain. KI696 blocks KEAP1-mediated ubiquitination and degradation of NRF2, promotes the translocation of NRF2 to the nucleus, activates the expression of downstream antioxidant genes, increases intracellular glutathione levels, and alleviates oxidative stress-induced cell damage and inflammatory cell infiltration in the lungs. KI696 reduces ozone-induced pulmonary oxidative damage and inflammatory cell accumulation in rats, and upregulates pulmonary antioxidant genes. KI696 can be used in research related to chronic obstructive pulmonary disease, oxidative stress and inflammation .
Cat. No.: HY-114118S3
Purity: 96.04%
Cat. No.: HY-121675A
CAS No.: 2855123-30-5
Synonyms: BOL-148 D-Tartrate; Bromolysergide D-Tartrate
Research Areas:
2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD D-Tartrate lacks 5-HT2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
Cat. No.: HY-13024A
CAS No.: 1033893-29-6
Synonyms: DCC-2036 tosylate
Research Areas:
Rebastinib tosylate (DCC-2036 tosylate) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC50 values of 0.8 nM and 4 nM against Abl1 WT and Abl1 T315I, respectively. Rebastinib tosylate potently inhibits CYP2C8 (IC50 = 0.0533 μM) and CYP2C9 (IC50 = 2.54 μM). Rebastinib tosylate allosterically inhibits Tie2 with an IC50 of 0.63 nM. Rebastinib tosylate inhibits the transcriptional activity of FoxO1. Rebastinib tosylate inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib tosylate induces Apoptosis. Rebastinib tosylate exerts anti-tumor activity in breast cancer. Rebastinib tosylate exerts anti-angiogenic effects. Rebastinib tosylate increases myotube diameter and improves reduced contractility. Rebastinib tosylate can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia .
Synonyms: DHEA sulfate sodium-d6; Prasterone sulfate sodium-d6
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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
