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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
1988 Results for "
effectively
" in MedChemExpress (MCE) Product Catalog:
Products (1988)
1988 Results for "effectively" in MCE Product Catalog:
Synonyms: (1R,9R)-DX8951f
Target:
Research Areas:
(1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
Cat. No.: HY-13631V
CAS No.: 2489613-15-0
Synonyms: (1R,9R)-DX-8951
Target:
Research Areas:
(1R,9R)-Exatecan ((1R,9R)-DX8951f) is a non-prodrug Camptothecin (HY-16560) derivative and a potent topoisomerase I (Topo I) inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan is (1S,9R)-Exatecan (HY-13631I).
Cat. No.: HY-146066A
Purity: 98.45%
Target:
Research Areas:
(R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1 (HY-146066). α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
Cat. No.: HY-171705
CAS No.: 1478585-60-2
Research Areas:
KMS99220 is an orally active, blood-brain barrier-permeable activator of the Nrf2 inhibitory protein Keap-1. KMS99220 enhances the activity of AMPK, activates the Nrf2 signaling pathway, and reduces the phosphorylation of IκB, nuclear translocation of NFκB, as well as the phosphorylation levels of JNK, IKK and p38 MAPK via HO-1. KMS99220 binds to Keap1 to trigger the nuclear translocation of Nrf2, induces the expression of HO-1, NQO1, GCLC, GCLM and proteasome subunits; enhances proteasomal enzymatic activity; inhibits iNOS expression, nitric oxide production and IL-1β generation; attenuates microglial activation; reduces α-synuclein aggregation; and prevents dopaminergic neuron degeneration and motor dysfunction. KMS99220 prevents the degeneration of dopaminergic neurons in the substantia nigra, induces the expression of Nrf2 downstream target genes, and effectively ameliorates associated motor dysfunction in a mouse model of Parkinson's disease. KMS99220 is applicable to research related to Parkinson's disease .
Cat. No.: HY-173132
CAS No.: 3114057-78-9
Research Areas:
AKR1Cs-IN-1 (Compound 29) is a potent and broad-spectrum inhibitor targeting members of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). By simultaneously occupying the SP2 and SP3 pockets, it effectively inhibits multiple isoforms and disrupts metabolic pathways associated with drug resistance. In enzymatic activity assays, AKR1Cs-IN-1 exhibited significant inhibitory potency, with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM against AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. In the doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, AKR1Cs-IN-1 showed remarkable resensitization effects and significantly enhanced the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on overcoming drug resistance in breast cancer .
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 .
Cat. No.: HY-179484
CAS No.: 2915282-32-3
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KRASG12C IN-19 is a selective and orally active KRAS G12C inhibitor. KRASG12C IN-19 exerts potent antiproliferative activity against the KRAS G12C-mutant non small cell lung cancer (NSCLC) cell line H358 with an IC50 of 7.6 nM, and effectively suppresses downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN 19 has no significant inhibitory activity against KRAS G12V and KRAS G12D-mutant cancer cells (PANC 1, Panc, AsPC 1, and GP2d cells) with IC50 > 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRAS G12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. KRASG12C IN 19 can be employed for research in KRAS G12C driven cancers, including non small cell lung cancer, pancreatic cancer, and colorectal cancer .
Cat. No.: HY-79602S
CAS No.: 1219795-34-2
Synonyms: p-Tosylamide-d4
Research Areas:
4-Tolyl-d4-sulfonamide (p-Tosylamide-d4) is the d4-labeled p-Toluenesulfonamide (HY-79602). p-Toluenesulfonamide is a small-molecule anticancer agent and plasticizer. p-Toluenesulfonamide exerts antitumor activity by inducing lysosomal membrane permeabilization, cathepsin B release and lysosome-mediated cell death. p-Toluenesulfonamide modulates cholesterol distribution in lipid rafts of tumor cell membranes and the Akt/mTOR/p70S6K pathway. p-Toluenesulfonamide shows activity against various cancers including hepatocellular carcinoma, non-small cell lung cancer and tongue squamous cell carcinoma; intrapleural injection effectively reduces malignant pleural effusion without causing pleural adhesion. p-Toluenesulfonamide is also the main degradation product of the disinfectant Chloramine-T (HY-B0959) in water. p-Toluenesulfonamide facilitates the localization of fluorescent probes to the endoplasmic reticulum. p-Toluenesulfonamide can be used in cancer-related research .
Cat. No.: HY-N0168AS1
CAS No.: 2750534-85-9
Cat. No.: HY-N0565AG
CAS No.: 10592-13-9
Cat. No.: HY-N0565BR
CAS No.: 24390-14-5
Synonyms: Doxycycline hydrochloride hemiethanolate hemihydrate (Standard); WC2031 (Standard)
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Doxycycline hyclate (Standard) is the analytical standard of Doxycycline hyclate (HY-N0565B). This product is intended for research and analytical applications. Doxycycline hyclate is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hyclate is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline hyclate also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hyclate induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline hyclate also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline hyclate has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers .
Cat. No.: HY-N0565S1
Cat. No.: HY-N5073
CAS No.: 178468-00-3
Synonyms: 4''-O-Glucosylvitexin
Cat. No.: HY-P2632C
Target:
Research Areas:
Cat. No.: HY-L242
495 compounds
Flavors and fragrances serve as indispensable enhancing elements in modern industries, playing multidimensional roles in the fields of food, cosmetics, and pharmaceutical development. In the food industry, flavors and fragrances are not only used to compensate for flavor loss during processing but also to create novel sensory experiences and enhance product appeal. Natural flavors such as vanilla and citrus oils impart rich, layered aromas to foods, while synthetic flavors can precisely replicate specific tastes, meeting the demands of standardized production and extending the flavor stability of food products. In the cosmetics sector, flavors and fragrances are key to emotional design. They enhance product recognition and elevate the pleasure of use through pleasant scents. In pharmaceutical development, the application of flavors and fragrances focuses on improving compliance. Especially in formulations such as oral liquids and chewable tablets, the addition of mint, fruit, and other flavoring components effectively masks the bitter or irritating taste of medications, increasing patient acceptance. Additionally, some natural flavors may themselves possess auxiliary therapeutic benefits.
MCE contains 495 kinds of flavors and fragrances, which can be used in fields such as food, cosmetics and drug development.
Cat. No.: HY-P992059
Cat. No.: HY-L209
1,992 compounds
The Ancient Chinese Classical Formulas, released by the State Administration of Traditional Chinese Medicine, selects the classic prescriptions from more than 100,000 prescriptions contained in more than 100 representative ancient medical books. Experts said that the classic prescription derived from ancient books, with thousands of years of human experience, is widely used in common diseases, frequented diseases, chronic diseases and other fields, and its development and utilization can fill the gap in medical drugs for some diseases in China, and effectively alleviate the increasingly severe medical needs brought by a series of social problems such as aging and chronic diseases in China. MCE has collected and sorted out these monomer compounds from the sources of ancient Chinese classical formulas, including licorice, ginseng, pinellia and other traditional Chinese medicine sources, which help to provide new ideas and new strategies for modern drug development.
MCE ancient Chinese classical formulas traditional Chinese medicine active compound library has 1,992 traditional Chinese medicine monomer compound, which can be used in the research fields of new drug development and drug target identification.
Cat. No.: HY-164729
Cat. No.: HY-L948
11,491 compounds
PD-1/PD-L1 are key immune checkpoint targets that suppress T-cell-mediated anti-tumor immunity, representing a major focus in cancer immunotherapy. While antibody drugs dominate the clinic, they are limited by administration challenges and immune-related side effects. Small-molecule PD-1/PD-L1 inhibitors, with oral availability, good tissue penetration and low cost, have emerged as a promising next-generation strategy.
A PD-1/PD-L1 lead-like library was built via a five-step virtual screening process. After collecting 8,947 inhibitors from BindingDB and PubChem and filtering by activity and duplicates, AI similarity screening was performed using GeminiMol. Key pharmacophores were extracted from the PPI interface of co-crystal structures, and molecular was screened via a pharmacophore model, effectively enhancing target activity.
Containing 10,000 structurally diverse and drug-like molecules well-matched to the PD-L1 pocket, the library supports virtual docking, high-throughput screening and hit discovery, enabling efficient and rapid development of small-molecule immunotherapies.
Cat. No.: HY-L135
3,540 compounds
With the progress of modern cancer therapy, the life of cancer patients has been extended. However, after initial treatment and recovery, the development of secondary tumors often leads to cancer recurrence. Cancer stem cells are a small number of cells that tumor growth and reproduction depend on.
Cancer stem cells have strong self-renewal ability, which is the direct cause of tumor occurrence. In addition, cancer stem cells also have the ability to differentiate into different cell types, playing a crucial role in tumor metastasis and development. Chemotherapy and radiotherapy induced DNA damage and apoptosis are common cancer treatments. However, cancer stem cells can effectively protect cancer cells from apoptosis by activating DNA repair ability. Cancer stem cells are regarded as the key "seed" of tumor occurrence, development, metastasis and recurrence. Since its first discovery in leukemia in 1994, cancer stem cells have been considered a promising therapeutic target for cancer treatment.
MCE supplies a unique collection of 3,540 compounds targeting key proteins in cancer stem cells. MCE Cancer Stem Cells Compound Library is a useful tool for cancer stem cells related research and anti-cancer drug development.
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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
