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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
2986 Results for "
broad
" in MedChemExpress (MCE) Product Catalog:
Products (2986)
2986 Results for "broad" in MCE Product Catalog:
Cat. No.: HY-L145
930 compounds
The majority of hypertensive patients have primary (or essential) hypertension, that is, hypertension in which secondary causes are not present. Management aims to control arterial pressure, prevent end-organ damage (cerebrovascular, cardiovascular, and renal), and reduce the risk of premature death.
Antihypertensive drugs may be divided into two broad groups, the first group being those which directly or indirectly block the renin–angiotensin system (RAS), for example, ACEIs, angiotensin receptor antagonists (ARAs), direct renin inhibitors (DRIs), and to a lesser extent β-blockers. The second group of drugs works by increasing water and sodium excretion, thereby reducing intravascular volume, or by causing vasodilatation through non-RAS pathways, for example, diuretics and calcium channel blockers (CCBs).
MCE offers a unique collection of 930 compounds with identified and potential antihypertensive activity. MCE Antihypertensive Compound Library is critical for antihypertensive drug discovery and development.
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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
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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-157804
CAS No.: 3029579-46-9
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PROTAC SARS-CoV-2 Mpro degrader-1 is a SARS-CoV-2 M pro PROTAC degrader with a DC50 of 18.1 μM. PROTAC SARS-CoV-2 Mpro degrader-1 recruits the Von-Hippel Lindau (VHL) E3 ligase to mediate ubiquitination and proteasomal degradation of SARS-CoV-2 M pro, without inhibiting the catalytic activity of M pro. PROTAC SARS-CoV-2 Mpro degrader-1 exhibits broad-spectrum antiviral activity against coronaviruses (SARS-CoV-2, HCoV-OC43, HCoV-229E). PROTAC SARS-CoV-2 Mpro degrader-1 can be used in studies related to SARS-CoV-2 infection, HCoV-OC43 infection, and HCoV-229E infection .
Cat. No.: HY-157805
CAS No.: 3057294-32-0
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PROTAC SARS-CoV-2 Mpro degrader-2 is a SARS-CoV-2 M pro PROTAC degrader with a DC50 of 1.34 μM. PROTAC SARS-CoV-2 Mpro degrader-2 recruits the VHL E3 ligase to mediate ubiquitination and proteasomal degradation of SARS-CoV-2 M pro, without inhibiting the catalytic activity of M pro. PROTAC SARS-CoV-2 Mpro degrader-2 exhibits anti-SARS-CoV-2 activity in infected cells, as well as broad-spectrum antiviral activity against coronaviruses including HCoV-OC43 and HCoV-229E. PROTAC SARS-CoV-2 Mpro degrader-2 can be used in studies related to SARS-CoV-2 infection, HCoV-OC43 infection, and HCoV-229E infection .
Cat. No.: HY-176283
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Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells .
Cat. No.: HY-179503
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Phosphodiesterase (PDE) TRP Channel NOD-like Receptor (NLR) NF-κB TNF Receptor Interleukin Related
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PDE/TRPA1/CHIT1-IN-1 is a phosphodiesterases (PDEs), TRPA1, and hCHIT1 (KD of 37.7 μM) inhibitor. PDE/TRPA1/CHIT1-IN-1 is a broad-spectrum PDE inhibitor, potently targeting key isoforms including PDE4B, PDE7A, PDE3A, and PDE8A with IC50s of 15.54, 15.15, 8.39 and 16.46 μM. PDE/TRPA1/CHIT1-IN-1 suppresses NLRP3 inflammasome activation and inhibits NF-κB phosphorylation, downregulating the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. PDE/TRPA1/CHIT1-IN-1 can be used for chronic obstructive pulmonary disease (COPD) and related inflammatory lung disorders research .
Cat. No.: HY-179556
SARS-CoV-2 nsp14-IN-10 is a highly potent and selective NSP14 (IC50 = 0.34 µM) S-adenosylmethionine (SAM) binding pocket inhibitor. SARS-CoV-2 nsp14-IN-10 demonstrates robust antiviral activity against SARS-CoV-2. SARS-CoV-2 nsp14-IN-10 exhibits broad-spectrum activity against other betacoronaviruses and inhibits SARS-CoV-2 at the replication stage. SARS-CoV-2 nsp14-IN-10 suppresses viral translation and exhibits immunostimulatory effects. SARS-CoV-2 nsp14-IN-10 specifically reverses NSP14-mediated alterations inhost transcriptome. SARS-CoV-2 nsp14-IN-10 can be used for the study of SARS-CoV-2 .
Cat. No.: HY-180269
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Anti-Influenza agent 10 (Compound 41) is an influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor. Anti-Influenza agent 10 exhibits potent antiviral activity against A/PR/8/34(H1N1) with an IC50 of 0.29μM and a KD of 4.11 μM. Anti-Influenza agent 10 can inhibit the assembly of the viral RdRp complex by disrupting the protein interaction between PA and PB1 subunits, thereby blocking the transcription and replication of the viral genome. Anti-Influenza agent 10 shows significant broad-spectrum effects on multiple influenza virus strains, such as H3N2, H3N8 and H9N2 with IC50 values of 3.96, 1.91 and 1.45 μM. Anti-Influenza agent 10 can be used for the research of influenza A Virus Infection .
Cat. No.: HY-181673
CAS No.: 3069681-35-9
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ICD inducer-2 is a immunogenic cell death inducer. ICD inducer-2 binds to the colchicine binding site on tubulin to inhibit tubulin polymerization. ICD inducer-2 exhibits broad-spectrum antiproliferative activity across multiple cancer cell lines. ICD inducer-2 inhibits cells migration, causes G2/M phase and induces apoptosis. ICD inducer-2 promotes infiltration of CD4+ and CD8+ T cells into the tumor microenvironment. ICD inducer-2 downregulates antiapoptotic protein Bcl-2, upregulates proapoptotic proteins Bax and Bim-1, and increases cleaved caspase 3, cleaved caspase 9, and cleaved PARP levels. ICD inducer-2 overcomes paclitaxel resistance in xenograft models and achieves tumor growth inhibition. ICD inducer-2 can be used for the research of cancer, such as lung carcinoma .
Cat. No.: HY-181687
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer .
Cat. No.: HY-18234B
CAS No.: 24365-47-7
Leupeptin Ac-LL is a broad-spectrum protease inhibitor . By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin Ac-LL significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin Ac-LL inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin Ac-LL can be used in research on chronic inflammatory diseases and skin tumorigenesis .
Cat. No.: HY-18234C
CAS No.: 24125-16-4
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Cat. No.: HY-189662
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Y-U0-S is a potent inhibitor of the coronavirus main protease (M pro) and host cathepsins. The IC50 values of Y-U0-S against SARS-CoV-2 M pro, SARS-CoV Mpro, Cathepsin B, and Cathepsin L are 0.81, 1.14, 0.86, and 21.13 μM, respectively. Y-U0-S exhibits broad-spectrum anti-coronavirus activity, with an EC50 of 0.22 μM against wild-type SARS-CoV-2. Y-U0-S forms an irreversible covalent bond with the catalytic site C145 of M pro through its aldehyde warhead, and by optimizing multi-site occupancy of the scaffold to engage conserved residues, it effectively blocks enzyme activity and inhibits viral replication. Y-U0-S can be used for research on COVID-19 .
Cat. No.: HY-B1953S
CAS No.: 1793071-39-2
Cat. No.: HY-N0565C
CAS No.: 94088-85-4
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Infection Neurological Disease Inflammation/Immunology Cancer
Doxycycline calcium is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline calcium 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 calcium also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline calcium 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 calcium 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 calcium has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers .
Cat. No.: HY-N0565D
CAS No.: 83038-87-3
Doxycycline fosfatex is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline fosfatex is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and fosfatex atoms. Doxycycline fosfatex also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline fosfatex 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 fosfatex 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 fosfatex has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers .
Cat. No.: HY-N20708
CAS No.: 89353-99-1
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Cat. No.: HY-N7101S
Synonyms: U-76-d7,252-d7; CS-807-d7
Cat. No.: HY-P10159
CAS No.: 1809102-71-3
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DJK-5 is an antimicrobial peptide that targets and degrades guanosine pentaphosphate and tetraphosphate (pppGpp and ppGpp). DJK-5 kills bacteria within dentinal tubules, dental plaque and preformed oral biofilms, delays biofilm recovery, reduces the abundance of extracellular polysaccharides and the structural integrity of biofilm matrices, and inhibits the formation and biomass accumulation of dental plaque biofilms. DJK-5 permeabilizes bacterial membranes, induces bacterial morphological changes, inhibits bacterial growth, and exerts a synergistic effect on bacterial biofilms when used in combination with traditional antibiotics and Colistin (HY-113678). DJK-5 exhibits protease resistance and broad-spectrum antibiofilm activity, though its activity decreases in fetal bovine serum. DJK-5 can be used in studies of pulpitis, mixed biofilm infections, skin abscesses, dental caries, infections associated with failed root canal therapy, and Pseudomonas aeruginosa biofilm-related respiratory tract infections .
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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
