Search Result
Results for "
human embryonic kidney cells
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-19907
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BMS-820836
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Dopamine Transporter
Monoamine Transporter
Serotonin Transporter
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Neurological Disease
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Liafensine (BMS-820836) is an orally active, blood-brain barrier-permeable monoamine reuptake inhibitor, with an IC50 of 5.67 nM against DAT, 1.08 nM against SERT, and 7.99 nM against NET. Liafensine binds to DAT to block dopamine reuptake. Liafensine binds to SERT to block serotonin reuptake. Liafensine binds to NET to block norepinephrine reuptake. Liafensine can be used in studies related to depression .
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- HY-N125722
-
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Aabomycin A1
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ATP Synthase
Antibiotic
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Infection
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Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
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- HY-B1482A
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TPS-23
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Potassium Channel
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Neurological Disease
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Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .
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- HY-P1684
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FOXP3 inhibitor P60
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NF-κB
Nuclear Factor of activated T Cells (NFAT)
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Infection
Inflammation/Immunology
Cancer
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Peptide P60 is a FOXP3 inhibitor. Peptide P60 reduces the nuclear translocation of FOXP3 and impairs FOXP3-mediated inhibition of NF-κB and NFAT activity. Peptide P60 inhibits the immunosuppressive activity of regulatory T cells and restores the proliferation and activation of effector T cells. Peptide P60 induces lymphoproliferative autoimmune syndrome in neonatal ICR mice and reduces the number of CD4 +CD25 +Foxp3 + T cells in the spleen. Peptide P60 enhances the efficacy of AH1 (HY-P4193) peptide vaccine and recombinant adenovirus-based HCV NS3 vaccine in BALB/c mice, including protective effects against CT26 tumor implantation. Peptide P60 can be used in studies related to tumor immunity, viral infection and lymphoproliferative autoimmune syndrome .
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- HY-162386
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Cuproptosis
Mitochondrial Metabolism
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Cancer
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UM4118 is a potent copper-selective non-genotoxic copper ionophore that induces cuproptosis in acute myeloid leukemia cells. UM4118 exhibits stronger activity against SF3B1G12C mutant acute myeloid leukemia cells. UM4118 transports extracellular copper into cells, elevates intracellular and mitochondrial copper levels, and triggers lipoylated DLAT aggregation, proteotoxic stress, iron-sulfur cluster protein depletion, reduced lipoylated protein levels, and maximal mitochondrial respiratory damage. UM4118 cytotoxicity can be enhanced by supplementation with extracellular copper, abolished by copper chelation, and shows synthetic lethal effects in the absence of iron-sulfur cluster biosynthesis/transport genes. UM4118 can be used for the study of acute myeloid leukemia .
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- HY-146369
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PROTACs
VEGFR
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Cancer
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PROTAC VEGFR-2 degrader-2 is a VEGFR-2 (KDR) PROTAC degrader with weak inhibitory activity against VEGFR-2 (IC50 > 1 μM). It is applicable to the research of cancer-related pathological angiogenesis .
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- HY-160645
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P2X Receptor
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Neurological Disease
Endocrinology
Cancer
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P2X4 antagonist-1 is a P2X4 receptor antagonist with an IC50 of 15 nM. P2X4 antagonist-1 inhibits ATP (HY-B2176)-induced calcium influx. P2X4 antagonist-1 can be used for the research of pain syndromes, endometriosis, cancer .
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- HY-103172
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P2Y Receptor
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Metabolic Disease
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8-Aminoadenine is an adenine receptor 1 (rAde1R) inhibitor with a Ki of 6.51 μM in rat and 0.0341 μM in human. 8-Aminoadenine inhibits isoprenaline-induced cAMP accumulation and adenine uptake in astrocytoma cells expressing rAde1R. 8-Aminoadenine serves as a lead structure for the development of adenine receptor ligands to elucidate the functions of the adenine receptor family .
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- HY-B1482
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TPS-23 benzenesulfonate
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Potassium Channel
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Neurological Disease
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Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders .
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- HY-117372
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TRP Channel
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Metabolic Disease
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DFL23448 is a selective transient receptor potential melastatin-8 (TRPM8) antagonist. DFL23448 shows IC50 values of 10 and 21 nM in hTRPM8 human embryonic kidney 293 cells activated by Cooling Agent 10 or cold. DFL23448 has limited activity (IC50 >10 μM) at transient receptor potential vanilloids TRPV1, TRPA1, or TRPV4 or at various G protein-coupled receptors. DFL23448 can modify bladder function and reduce bladder overactivity in awake rats .
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- HY-W033728
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Bacterial
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Infection
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Platinum(COD)dichloride (Compound Pt1) is an Antibacterial agent. Platinum(COD)dichloride shows antibacterial activity against a panel of gram-positive bacteria including Vancomycin (HY-B0671) and Methicillin (HY-121544) resistant Staphylococcus aureus .
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- HY-P10858
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SARS-CoV
Virus Protease
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Infection
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UCI-1 is a SARS-CoV-2 main protease (M pro) cyclic peptide inhibitor with an IC50 of 160 μM. UCI-1 shows no obvious cytotoxicity at the concentration of inhibiting M pro. UCI-1 can be used in the study of anti-COVID-19 drugs .
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- HY-167835A
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Bacterial
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Infection
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Tembetarine chloride is a alkaloid that can be isolated from Tinospora cordifolia that exhibits antibacterial activity. Tembetarine chloride exhibits weak cytotoxicity against mouse fibroblasts (L929) and human embryonic kidney cells (HEK293) with IC50 of 1245.33 μg/mL and 1642.81 μg/mL, respectively .
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- HY-B1482AS
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Isotope-Labeled Compounds
Potassium Channel
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Neurological Disease
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Mesoridazine-d3 is the deuterium labeled Mesoridazine (HY-B1482A). Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .
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- HY-155707
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Dopamine Receptor
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Inflammation/Immunology
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MOR agonist-3 (Compound 84) is a D3R/MOR antagonist/partial agonist a(Ki 382 nM and 55.2 nM respectively). MOR agonist-3 has the potential to produce analgesic effects through MOR (μ-opioid receptor) (HY-149337) partial agonists. MOR agonist-3 can be used in the inflammation and neuropathic pain research .
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- HY-181116
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CDK
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Cancer
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Anticancer agent 298 is a bi-nuclear Cu(II)-hydrazone complexe. Anticancer agent 298 can bind to the CDK-2 active site (PDB ID: 3IG7) via hydrogen bonds with key amino acid residues. Anticancer agent 298 exerts cytotoxic effects against hepatocellular carcinoma cells, and has lower cytotoxicity against normal human embryonic kidney cells. Anticancer agent 298 can be used for the research of hepatocellular carcinoma .
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- HY-125217
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PARP
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Cancer
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PARP10-IN-1 is a PARP10 inhibitor with an IC50 of 1.8 μM, 2.7 μM, and >10-fold selectivity over most PARP family members, excluding PARP7 and PARP16.PARP10-IN-1 inhibits PARP10-mediated mono-ADP-ribosylation, including auto-MARylation of PARP10 and MARylation of its protein targets.PARP10-IN-1 is membrane permeable and inhibits PARP10-dependent MARylation in human embryonic kidney cells.PARP10-IN-1 can be used for the research of cancer .
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- HY-182636
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Deubiquitinase
Aldehyde Dehydrogenase (ALDH)
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Metabolic Disease
Inflammation/Immunology
Cancer
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MT16-001 is a cell-permeable UCHL1 inhibitor with an IC50 value of 580 nM. MT16-001 also exhibits considerable inhibitory activity against USP30, and shows selectivity for other UCH family deubiquitinases (DUBs) as well as the broader proteome. MT16-001 binds covalently to the cysteine residue at the active site of UCHL1, and forms covalent interactions with ALDH2, ALDH9A1 and GATD3A in intact cells. Meanwhile, as a cytotoxic agent, it displays a steep dose-response curve in human embryonic kidney cells. MT16-001 can be used for research on various cancers, liver fibrosis and pulmonary fibrosis .
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- HY-181154
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PROTACs
SARS-CoV
Virus Protease
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Infection
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PROTAC SARS-CoV-2 Mpro degrader-5 is a SARS-CoV-2 main protease (Mpro) PROTAC. PROTAC SARS-CoV-2 Mpro degrader-5 engages CRBN E3 ubiquitin ligase to form a ternary complex with SARS-CoV-2 Mpro, induces K48-linked polyubiquitination of SARS-CoV-2 Mpro, and drives proteasome-dependent turnover of SARS-CoV-2 Mpro with a high selectivity index (CC50/DC50 > 10) in human embryonic kidney cells.PROTAC SARS-CoV-2 Mpro degrader-5 can be used for the research of COVID-19 .
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- HY-N19756
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RAR/RXR
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Cancer
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Cochinchinone P is a retinoid X receptor-α (RXRα) inhibitor that inhibits 9-cis-retinoic acid (HY-15128)-induced transcriptional activity of RXRα in vitro. Cochinchinone P can be used in cancer research .
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- HY-135435
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VEGFR
PDGFR
FGFR
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Neurological Disease
Metabolic Disease
Cancer
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SU10944 is a selective, orally active VEGFR inhibitor, with an IC50 of 6 nM against VEGFR-1, an IC50 of 96 nM and a Ki of 21 nM against VEGFR-2. SU10944 only exhibits weak inhibitory activity against PDGFRβ (IC50 = 1 μM), SCFR (IC50 = 1.58 μM) and FGFR-1 (IC50 = 1.6 μM). SU10944 selectively inhibits VEGFR receptor downstream signaling, neovascularization, vascular permeability, VEGF-mediated tissue factor production, and induces tumor growth delay. SU10944 can be used in research related to diabetic retinopathy, exudative age-related macular degeneration or cancer .
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- HY-W1135319
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Casein Kinase
Wee1
IKZF Family
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Cancer
|
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SB-405483 is a CRBN orthosteric ligand bindign enhancer. SB-405483 potentiates degradation of CRBN substrates including CK1α, Wee1, IKZF1/3. SB-405483 stabilizes CRBN and reduces CRBN autoubiquitination. SB-405483 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia .
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- HY-183692
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FXR
G protein-coupled Bile Acid Receptor 1
TNF Receptor
Heme Oxygenase (HO)
Quinone Reductase
Keap1-Nrf2
|
Cardiovascular Disease
Inflammation/Immunology
|
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FXR agonist 18 is an orally active FXR agonist, with an EC50 of 10 nM against human FXR and an EC50 of 1360 nM against human TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis .
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- HY-W269285
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D-1,2,3,4-Tetrahydronorharman-3-carboxylic acid
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Drug Derivative
NO Synthase
Cytochrome P450
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Cancer
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H-D-Tpi-OH is a tetrahydro-β-carboline derivative. H-D-Tpi-OH only slightly upregulates QR1, mildly inhibits the aromatase and NO synthesis pathways, and shows no significant in vitro anti-breast tumor proliferation activity. H-D-Tpi-OH can be used in cancer-related research .
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- HY-183698
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CDK
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Cancer
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CDK9-IN-51 is a CDK9 inhibitor. CDK9-IN-51 binds stably to purified CDK9 protein via interactions with key active-site residues Cys106, Asp109, and Phe103. CDK9-IN-51 exhibits antiproliferative activity against multiple cancer cells. CDK9-IN-51 can be used for the research of cancer, such as lung carcinoma, cervical carcinoma and breast carcinoma .
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- HY-183326
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IDMF
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Keap1-Nrf2
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Inflammation/Immunology
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Isosorbide di-(methyl fumarate) (IDMF), topical DMF (HY-17363) derivative, is an NRF2/ARE pathway activator. Isosorbide di-(methyl fumarate) downregulates ANCR targets, modulates epithelial differentiation, represses proinflammatory cytokine genes, IL-17A- and TNF-induced keratinocyte genes, psoriatic skin lesion-specific genes, and immune response genes. Isosorbide di-(methyl fumarate) stimulates oxidative stress response gene transcription, reduces erythema and scaling in Imiquimod (HY-B0180)-induced psoriasiform lesions. Isosorbide di-(methyl fumarate) exhibits no genotoxicity or radiation sensitivity in skin fibroblasts, is nonirritating and nonsensitizing in rodent models. Isosorbide di-(methyl fumarate) can be used for the research of psoriasis vulgaris .
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- HY-P11622
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Drug Derivative
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Infection
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Gramicidin S analogue 9 is a bactericidal agent that can be found as a cyclic peptide analogue. Gramicidin S analogue 9 disrupts bacterial cell membranes. Gramicidin S analogue 9 can be used for the research of methicillin-resistant staphylococcus aureus infection .
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- HY-N19113
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Endogenous Metabolite
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Infection
Cancer
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Emindole SB is an anticancer agent. Emindole SB can be isolated from Penicillium species. Emindole SB exerts anticancer effects against ovarian cancer, breast cancer and lymphoma. Emindole SB shows no toxicity to Caenorhabditis elegans. Emindole SB can be used in studies related to ovarian cancer, lymphoma and breast cancer .
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- HY-182308
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Interleukin Related
TNF Receptor
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Inflammation/Immunology
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LC-PDA-01 is a selective peroxiredoxin 1 (PRDX1) activator with an EC50 of 111.8 nM and a human KD of 123.2 nM. LC-PDA-01 inhibits the expression of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α. LC-PDA-01 can be used in antioxidant/anti-inflammatory research .
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- HY-181940
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Proteasome
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Cancer
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Berberine-amide-m-PhBA chloride (Compound 8b) is a selective anti-breast cancer agent. Berberine-amide-m-PhBA chloride may inhibit the proteasome by interacting with the 20S proteasome β5 subunit. Berberine-amide-m-PhBA chloride can be used in the research of breast cancer .
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- HY-182510
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STAT
Interleukin Related
Apoptosis
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Cancer
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NTZ-24 is a selective STAT3 pathway inhibitor. NTZ-24 suppresses STAT3 phosphorylation at Tyr705, blocks STAT3-DNA interaction, and downregulates the levels of STAT3 downstream target proteins. NTZ-24 induces cell-cycle arrest and promotes apoptosis in cancer cells. NTZ-24 exerts significant antiproliferative activity against HeLa cells (IC50 = 3.3 μM). NTZ-24 can be used for the research of cervical cancer .
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- HY-W034984
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Bacterial
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Infection
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(1,5-Cyclooctadiene) dimethylplatinum (II) (Compound Pt3) is an Antibacterial agent. (1,5-Cyclooctadiene) dimethylplatinum (II) exhibits limited but selective activity against some Gram-positive Staphylococcus aureus strains, including methicillin-resistant Staphylococcus aureus (MRSA) and Glycopeptide-intermediate Staphylococcus aureus (GISA). (1,5-Cyclooctadiene) dimethylplatinum (II) shows no hemolytic activity .
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- HY-182346
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FBPase
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Metabolic Disease
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FBPase-IN-7 is a fructose-1,6-bisphosphatase (FBPase) inhibitor with an IC50 of 0.75 μM. FBPase-IN-7 binds to a cryptic allosteric pocket of FBPase, induces conformational rearrangement of key residues, forms a hydrogen-bond network, and disrupts substrate catalysis. FBPase-IN-7 confirms cellular stabilizes HuFBPase in hepatic cells. FBPase-IN-7 has hypoglycemic activity. FBPase-IN-7 can be used for the research of type 2 diabetes .
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- HY-181923
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EGFR
CDK
Cytochrome P450
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Cancer
|
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IMP-Zn is a pyrazole-hydrazone Schiff base zinc (II) complex. IMP-Zn exhibits significant antiproliferative activity against human colorectal cancer cells and induces cell cycle arrest. IMP-Zn shows stronger binding affinity than its free ligand IMP towards three cancer-related protein targets: EGFR kinase 1M17, cytochrome P450 3RUK, and CDK inhibitor 6GUE. IMP-Zn can be used in studies related to colorectal cancer .
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- HY-181266
-
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Parasite
Aminopeptidase
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Infection
|
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Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with Ki values of 27 nM and 81 nM, respectively. Antimalarial agent 55 exhibits potent nanomolar activity against homologous enzymes from Plasmodium vivax and Plasmodium berghei, with Ki values of 2 nM, 4 nM, 190 nM and 18 nM for Pv-M1, Pb-M1, Pv-M17 and Pb-M17, respectively. Antimalarial agent 55 possesses significant antiplasmodial activity, as well as cross-species inhibitory capacity and broad-spectrum activity that is unaffected by existing drug resistance mechanisms. Antimalarial agent 55 can be used in malaria research .
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- HY-182589
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FAAH
Potassium Channel
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Neurological Disease
Metabolic Disease
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|
SRP-001 is an orally active, blood-brain barrier-permeable analgesic and antipyretic agent. SRP-001 reduces the expression level of FAAH, mildly inhibits hERG currents, generates AM404 (HY-101388), and maintains the integrity of hepatic tight junctions. SRP-001 exerts analgesic, antipyretic, and antinociceptive effects .
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- HY-182539
-
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CGRP Receptor
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Others
Neurological Disease
|
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DD04107 is a neuronal exocytosis inhibitor with a rat Syt1-C2B domain binding Ka of 2.4 μM. DD04107 interferes with synaptobrevin-syntaxin-SNAP-25 complex formation and Syt1-SNARE complex interaction to block α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons. DD04107 blocks inflammatory ion channel recruitment to nociceptor plasma membranes. DD04107 can be used for the research of chronic inflammatory pain, neuropathic pain, osteosarcoma pain, chemotherapy-induced peripheral neuropathy, diabetic neuropathy, inflammatory pain .
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-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1684
-
|
FOXP3 inhibitor P60
|
NF-κB
Nuclear Factor of activated T Cells (NFAT)
|
Infection
Inflammation/Immunology
Cancer
|
|
Peptide P60 is a FOXP3 inhibitor. Peptide P60 reduces the nuclear translocation of FOXP3 and impairs FOXP3-mediated inhibition of NF-κB and NFAT activity. Peptide P60 inhibits the immunosuppressive activity of regulatory T cells and restores the proliferation and activation of effector T cells. Peptide P60 induces lymphoproliferative autoimmune syndrome in neonatal ICR mice and reduces the number of CD4 +CD25 +Foxp3 + T cells in the spleen. Peptide P60 enhances the efficacy of AH1 (HY-P4193) peptide vaccine and recombinant adenovirus-based HCV NS3 vaccine in BALB/c mice, including protective effects against CT26 tumor implantation. Peptide P60 can be used in studies related to tumor immunity, viral infection and lymphoproliferative autoimmune syndrome .
|
-
- HY-P10858
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
UCI-1 is a SARS-CoV-2 main protease (M pro) cyclic peptide inhibitor with an IC50 of 160 μM. UCI-1 shows no obvious cytotoxicity at the concentration of inhibiting M pro. UCI-1 can be used in the study of anti-COVID-19 drugs .
|
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- HY-P11622
-
|
|
Drug Derivative
|
Infection
|
|
Gramicidin S analogue 9 is a bactericidal agent that can be found as a cyclic peptide analogue. Gramicidin S analogue 9 disrupts bacterial cell membranes. Gramicidin S analogue 9 can be used for the research of methicillin-resistant staphylococcus aureus infection .
|
-
- HY-182539
-
|
|
CGRP Receptor
|
Others
Neurological Disease
|
|
DD04107 is a neuronal exocytosis inhibitor with a rat Syt1-C2B domain binding Ka of 2.4 μM. DD04107 interferes with synaptobrevin-syntaxin-SNAP-25 complex formation and Syt1-SNARE complex interaction to block α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons. DD04107 blocks inflammatory ion channel recruitment to nociceptor plasma membranes. DD04107 can be used for the research of chronic inflammatory pain, neuropathic pain, osteosarcoma pain, chemotherapy-induced peripheral neuropathy, diabetic neuropathy, inflammatory pain .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B1482AS
-
|
|
|
Mesoridazine-d3 is the deuterium labeled Mesoridazine (HY-B1482A). Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells .Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders .
|
-
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