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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
9515 Results for "
ester derivative
" in MedChemExpress (MCE) Product Catalog:
Products (9515)
9515 Results for "ester derivative" in MCE Product Catalog:
Cat. No.: HY-14988
CAS No.: 1143579-76-3
I-A09 and its derivatives, specifically 1,2,3-triazole-adamantylacetamide hybrids (5a–u), exhibit significant antitubercular activity. These hybrids were synthesized using copper-catalyzed click chemistry, combining bioactive fragments from antitubercular I-A09 and substituted adamantyl urea. The compound N-(1-adamantyl)-2-azido acetamide was reacted with various alkyl/aryl acetylenes to produce new analogues. Among them, N-(1-adamantan-1-yl)-2-(4-(phenanthren-2-yl)-1H-1,2,3-triazol-1-yl)acetamide (5t) showed the most promise with a minimum inhibitory concentration (MIC) of 3.12 μg/mL against Mycobacterium tuberculosis H37Rv, and a selectivity index greater than 15 .
Cat. No.: HY-15026
CAS No.: 915798-75-3
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ATB-429, a novel H2S-releasing derivative of mesalamine, demonstrates significant anti-nociceptive and anti-inflammatory effects in models of irritable bowel syndrome (IBS). By releasing hydrogen sulfide (H2S), ATB-429 modulates colorectal distension-induced hypersensitivity in both healthy and postcolitic rats. It attenuates abdominal withdrawal responses and suppresses spinal c-Fos mRNA expression, indicating its potential to alleviate pain associated with gastrointestinal inflammation. Moreover, ATB-429 down-regulates colonic cyclooxygenase-2 and interleukin-1β mRNA expression, effects not observed with mesalamine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, as evidenced by reversal of ATB-429's effects with glibenclamide. These findings suggest ATB-429 could offer therapeutic benefits for managing painful intestinal disorders linked to inflammation .
Cat. No.: HY-151833
CAS No.: 2639395-39-2
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Methyltetrazine-amido-N-bis(PEG4-acid) is a click chemistry reagent containing an azide group. Methyltetrazine-amido-N-bis(PEG4-acid) is a PEG derivative that contains a methyltetrazine group and two acid groups. This reagent can react with TCO-containing compounds to form a stable covalent bond without the catalysis of Cu or elevated temperatures. The inverse-electron demand Diels-Alder cycloaddition reaction of TCO with tetrazines is the fastest bioorthogonal reaction with exceptional selectivity. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. PEG linker increases the water solubility of the compound. Reagent grade, for research use only . Methyltetrazine-amido-N-bis(PEG4-acid) is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.
Cat. No.: HY-154825
CAS No.: 651734-12-2
Synonyms: 20(OH)D3; 20S-Hydroxyvitamin D3
Research Areas:
20-Hydroxyvitamin D3 (20(OH)D3), a product of vitamin D3 hydroxylation, is a noncalcemic immunomodulator. 20-Hydroxyvitamin D3 binds to vitamin D receptor (VDR), activates VDR and aryl hydrocarbon receptor (AhR) signaling, stimulates CYP24A1 expression, and drives VDR nuclear translocation. 20-Hydroxyvitamin D3 inhibits NF-κB activity via IκBα upregulation. 20-Hydroxyvitamin D3 acts as a substrate for CYP27B1 and rat CYP24A1, undergoing hydroxylation to form dihydroxy-derivatives. 20-Hydroxyvitamin D3 inhibits cell proliferation, colony formation, migration, and tumor growth, and induces cell differentiation in cancer cells. 20-Hydroxyvitamin D3 can be used for the research of inflammatory and autoimmune diseases, melanoma, breast carcinomas, and hepatocarcinoma .
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PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (Kd = 8.2 μM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo .
Cat. No.: HY-162815
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PROTAC SMARCA2/4 degrader-26 is a SMARCA2/4 PROTAC degrader with selective anti-tumor activity against lung cancer cells. PROTAC SMARCA2/4 degrader-26 degrades SMARCA2 and SMARCA4 via the PROTAC-mediated proteasomal pathway. It induces DNA damage and apoptosis in tumor cells, while inhibiting migration and colony formation of lung cancer cells; in addition, it damages normal vascular endothelial cells and exhibits significant off-target-related cytotoxicity. PROTAC SMARCA2/4 degrader-26 serves as the parent scaffold to construct the GSH-responsive prodrug PROTAC SMARCA2/4 degrader-25 (HY-162813), a derivative that shows drastically reduced cytotoxicity against normal cells. PROTAC SMARCA2/4 degrader-26 can be used in lung cancer-related research .
Cat. No.: HY-180767
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Azithromycin-amide-C3-amide-quinoxaline (Compound 5f) is an Azithromycin (HY-17506) derivative and antibacterial agent. Azithromycin-amide-C3-amide-quinoxaline inhibits topoisoisomerase I with an IC50 of 120.7 μM. Azithromycin-amide-C3-amide-quinoxaline interacts with 70S E. coli ribosome with a Kd of 0.8 nM. Azithromycin-amide-C3-amide-quinoxaline inhibits bacterial translation with an IC50 of 0.7 μM. Azithromycin-amide-C3-amide-quinoxaline shows antibacterial potency against S. pneumonia ATCC 49619, S. aureus ATCC 29213, E. faecalis ATCC 29212 with MICs of 0.06 μg/mL, 2 μg/mL, 0.5 μg/mL, respectively. Azithromycin-amide-C3-amide-quinoxaline exhibits anticancer activity against prostate cancer, colon cancer .
Cat. No.: HY-184265
CAS No.: 1993461-76-9
Synonyms: Mito-Esc
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
Mito-Esculetin (Mito-Esc) is an orally active mitochondria-targeted derivative of Esculetin (HY-N0284). Mito-Esculetin inhibits LPS-induced phosphorylation of STAT3 Tyr-705, partially reverses LPS-mediated depletion of SIRT3, and enhances the AMPK-SIRT1 signaling axis. Mito-Esculetin inhibits PAI-1 activity, regulates miRNA, and induces phosphorylation of IRS and AKT. Mito-Esculetin suppresses oxidant-induced endothelial dysfunction, Ang-II (HY-13948)- and high glucose-induced atherosclerotic plaque formation, Palmitate (HY-N0830)-induced insulin resistance, as well as high glucose-mediated endothelial cell senescence and inflammatory responses. Mito-Esculetin reduces body weight and non-esterified fatty acid (NEFA) levels. Mito-Esculetin can be used in research related to acute coronary syndrome, type 2 diabetes, and hyperglycemia-induced atherosclerosis .
Cat. No.: HY-184620
Ferric oxide (Fe3O4) is widely used in magnetic resonance imaging (MRI), magnetic separation, targeted drug delivery, tumor hyperthermia, cell labeling and separation, and as a contrast agent and enhancement agent in retinal detachment repair surgery due to its stable material properties, good biocompatibility, high strength, and lack of toxic side effects. It is also used as a catalyst carrier, microwave absorbing material, and magnetic recording material. Xianfeng has developed numerous derivatives of ferric oxide, including oleic acid-modified ferric oxide, PEG-terminated ferric oxide, DMSA-modified ferric oxide, polylysine-modified ferric oxide, carboxylated dextran-modified ferric oxide nanoparticles, streptavidin-modified ferric oxide particles, thiol-modified ferric oxide magnetic nanoparticles, and polyethyleneimine (PEI)-modified magnetic ferric oxide nanoparticles, among others. This wide range of modifications provides numerous options for subsequent experiments.
Cat. No.: HY-184737
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Drug Derivative Bcl-2 Family Caspase PARP Mitochondrial Metabolism ATP Synthase Reactive Oxygen Species (ROS) Apoptosis
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TPP-C8-CO-DSG bromide is a derivative of Diosgenin (HY-N0177) and an anticancer agent. TPP-C8-CO-DSG bromide downregulates Bcl-2 expression and upregulates Bax expression. TPP-C8-CO-DSG bromide promotes the cleavage of Caspase 9, Caspase 3 and PARP-1. TPP-C8-CO-DSG bromide depolarizes mitochondrial membrane potential, reduces intracellular ATP production, and induces intracellular ROS accumulation. TPP-C8-CO-DSG bromide promotes Apoptosis. TPP-C8-CO-DSG bromide exhibits anticancer activity against prostate cancer, breast cancer, lung adenocarcinoma, cervical cancer and colorectal cancer. TPP-C8-CO-DSG bromide can be used in the research of cervical cancer .
Synonyms: D-(+)-Camphor (Standard); (1R)-(+)-Camphor (Standard)
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Cat. No.: HY-D0077
CAS No.: 195136-58-4
Synonyms: Oregon green 488
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2',7'-Difluorofluorescein (Oregon green 488) is a fluorescein derivative and a pH-sensitive fluorescent probe (pKa ~4.7). Upon excitation at 488 nm, 2',7'-Difluorofluorescein exhibits pH-sensitive fluorescence intensity through the formation of dianions, while its pH sensitivity decreases under excitation at 450 nm, allowing its use in ratiometric pH analysis. 2',7'-Difluorofluorescein can be used for the quantitative analysis of pH values in the range of 2-7 in submicron aerosol particles. 2',7'-Difluorofluorescein undergoes buffer-mediated and buffer-free excited-state proton transfer between different protonated forms, and its cationic form undergoes rapid excited-state deprotonation. 2',7'-Difluorofluorescein is resistant to photodegradation, maintains stable absorption and fluorescence properties within the physiological pH range, and serves as a fluorescent protein label, a component of Ca 2+ indicators, a fluorescent imaging agent, and an anisotropy probe .
Cat. No.: HY-D1850
Cat. No.: HY-D3074
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TCM-4COOH is an AIE-active fluorescent probe for calcium ions. TCM-4COOH relies on aggregation-induced emission activity, and its carboxyl chelating group can bind to Ca 2+ and Mg 2+ to form insoluble aggregates, triggering fluorescence enhancement via restricting intramolecular motion (Ex/Em = 477/603 nm). TCM-4COOH shows pH independence in physiological environments (pH 4-9), can be strongly activated at Ca 2+ concentrations ranging from low nM to mM, and has a stronger binding ability to Ca 2+ than to Mg 2+. TCM-4COOH, as its acetoxymethyl ester derivative TCM-AM, can penetrate cell membranes for intracellular detection. TCM-4COOH can be used for imaging of cellular calcium overload, detection of bone microcracks, and studies related to calcium-rich biological environments .
Cat. No.: HY-N16818
CAS No.: 1242672-31-6
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Cat. No.: HY-N2492R
CAS No.: 19367-38-5
Synonyms: Methyl trans-p-coumarate (Standard)
Cat. No.: HY-W001952
CAS No.: 15231-91-1
Cat. No.: HY-W006886
CAS No.: 945212-26-0
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Cat. No.: HY-120914
CAS No.: 170950-29-5
Synonyms: GO-Y015
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Glutathione Peroxidase Keap1-Nrf2 Heme Oxygenase (HO) Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism Drug Derivative TrxR
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TrxR1-IN-B19 (GO-Y015) is a Curcumin (HY-N0005) derivative and TrxR1 inhibitor. TrxR1-IN-B19 inhibits de novo selenoprotein synthesis, suppresses SeP and GPx expression, and impairs selenium incorporation into Sec-tRNA[Sec]. TrxR1-IN-B19 induces Nrf2 accumulation through Keap1 cysteine modification, HO-1 expression, GSH synthesis, ROS accumulation, ER stress, mitochondrial dysfunction, Apoptosis, and G2/M phase arrest. TrxR1-IN-B19 improves glucose tolerance and insulin sensitivity, lowers blood glucose, inhibits tumor growth, and reduces arsenic accumulation. TrxR1-IN-B19 can be used for research on type 2 diabetes, arsenite-induced toxicity, and gastric cancer .
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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
