Search Result
Results for "
knockout
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W747072
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3-Sulfocholyl Taurine; TCA3S
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Drug Metabolite
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Metabolic Disease
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3-Sulfo-taurocholic Acid Disodium Salt (3-Sulfocholyl Taurine; TCA3S) is a metabolite of the conjugated bile acid taurocholic acid. Plasma levels of 3-Sulfo-taurocholic Acid Disodium Salt are elevated in wild-type and Sortilin 1 (Sort1) knockout mice at 6 hours following bile duct ligation (BDL) and are further elevated in Sort1 knockout mice at 24 hours post-BDL.
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- HY-136057
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Ferroptosis
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Cancer
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iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A) .
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- HY-160887
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5-HT Receptor
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Neurological Disease
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FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models .
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- HY-19914
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- HY-161246
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5-HT Receptor
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Neurological Disease
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uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
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- HY-P991477
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CXCR
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Inflammation/Immunology
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HFB-100204 is a human monoclonal antibody (mAb) targeting CXCR5. HFB-100204 reduces CXCR5+ immune cells, including B cells and Tfh cells, in the blood and spleen of hCXCR5 knockout mice. HFB-100204 can be used in autoimmune diseases research .
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- HY-P5437
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PKC
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Others
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PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
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- HY-172371
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Reactive Oxygen Species (ROS)
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Others
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Hypoxystat increases the affinity of hemoglobin for oxygen and reduces the release of oxygen to tissues, thereby inducing the tissue hypoxia. Hypoxystat alleviates the mitochondrial disease Leigh syndrome in Ndufs4 knockout mouse models. Hypoxystat exhibits orally activity .
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- HY-149611
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Monoamine Oxidase
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Cancer
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Lysyl hydroxylase 2-IN-2 (compound 13) is a potent Lysyl hydroxylase 2 (LH2) inhibitor, with the IC50 of approximately 500 nM. Lysyl hydroxylase 2-IN-2 inhibits the migration in 344SQ WT cells, but not impedes the migration of the same cell line with an LH2 knockout cells .
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- HY-159910
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Mitochondrial Metabolism
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Cancer
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LH1513 is a dioxalate derivative of l-lysine (HY-N0469) that inhibits CaOx crystallization with better activity than citrate and pyruvate. LH1513 has potential preventive activity in hyperoxaluria models and effectively prevents urinary CaOx crystal formation in Agxt knockout mice. AGXT-1 is a mitochondrial protein involved in metabolism .
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- HY-148764
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Apoptosis
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Cancer
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M47 is a small molecule that selectively destabilizes Cryptochrome 1 (CRY1) and increases degradation of the CRY1 in the nucleus. M47 enhances apoptosis in Ras-transformed P53-deficient mouse skin fibroblast lines and enhances life span in p53 knockout mice. M47 can be used in research of cancer .
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- HY-117764
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mGluR
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Neurological Disease
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LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .
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- HY-16950
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(Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen; (Z)-Afimoxifene
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Estrogen Receptor/ERR
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Cancer
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4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is an orally active, selective estrogen receptor modulator (SERM). 4-Hydroxytamoxifen ((Z)-4-Hydroxytamoxifen) is also the active metabolic form of Tamoxifen (HY-13757A) in vivo and can be used to induce gene knockout in transgenic mice expressing CreER .
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- HY-111287
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DK-1-49
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Autophagy
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Cancer
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Autophagonizer (DK-1-49) is a small molecule autophagy inducer that results in an accumulation of autophagy-associated LC3-II and enhances levels of autophagosomes and acidic vacuoles. Autophagonizer inhibits cell viability and induces cell death in not only cancer cells but also Bax/Bak double-knockout cells with EC50 values of 3-4 μM .
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- HY-108786
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ENB-0040
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Phosphatase
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Metabolic Disease
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Asfotase alfa (ENB-0040) is a bone-targeted genetically engineered glycoprotein. Asfotase alfa increases the survival rate, bone mineralization and bone length and prevents mineralization defects of the feet, rib cage, lower limbs, jaw bones in Akp2 / knockout mice. Asfotase alfa can be used for the research of perinatal, infantile, and juvenile-onset hypophosphatasia (HPP) .
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- HY-P10680
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Liposome
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Others
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TFE-IDAtp1-LinA is a highly potent amphiphilic carrier, containing a trifluoroethyl-iminodiacetic acid analog of Stp. TFE-IDAtp1-LinA, formed nanoparticles with Cas9 RNP/ssDNA, achieved enhanced green fluorescent protein knockouts with an ED50 of 0.38 nM Cas9/sgRNA ribonucleoproteins (RNP) .
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- HY-103259
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- HY-W288951
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PKA
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Metabolic Disease
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FMP-API-1 is an A-kinase anchoring protein (AKAP)-PKA interaction inhibitor. FMP-API-1 binds to the allosteric site of PKA R subunits and increases the activity of PKA and AQP2 in PKA-knockout cell lines of renal cortical collecting ducts (mpkCCD cells). FMP-API-1 has the potential for the study of nephrogenic diabetes insipidus (NDI) .
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- HY-161671
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nAChR
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Neurological Disease
Inflammation/Immunology
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GAT2711 is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice .
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- HY-145272
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ELOVL
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Neurological Disease
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ELOVL1-IN-3 (Compound 22) is a potent and orally active inhibitor of elongation of very long chain fatty acid 1 (ELOVL1) enzyme. ELOVL1-IN-3 serves as a useful tool for researching adrenoleukodystrophy (ALD) [1].
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- HY-16968
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15-PGDH
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Others
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SW033291 is a potent and high-affinity inhibitor of 15-PGDH with a Ki of 0.1 nM. SW033291 increases prostaglandin PGE2 levels in bone marrow and other tissues. SW033291 also promotes tissue regeneration .
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- HY-135555
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5-CT
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5-HT Receptor
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Neurological Disease
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5-Carboxamidotryptamine (5-CT) is a 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, 5-HT7 receptor agonist . 5-Carboxamidotryptamine has a Ki value of 4.6 nM for cloned human 5-HT5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice .
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- HY-154979
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DNA/RNA Synthesis
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Inflammation/Immunology
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Anti-hepatic fibrosis agent 2 (Compound 6k) is an orally active COL1A1 inhibitor. Anti-hepatic fibrosis agent 2 is an anti-fibrogenic agent targeting ewing sarcoma breakpoint region 1 (EWSR1) .
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- HY-171272
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Reactive Oxygen Species (ROS)
MDM-2/p53
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Cancer
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PRDX1-IN-3 (compound 19-048) is a PRDX1 covalent inhibitor with anti-colorectal cancer activity. PRDX1-IN-3 can effectively inhibit the proliferation of colorectal cancer cells, and its antitumor effect on nude mice with colorectal cancer carrying PRDX1 gene knockout is significantly reduced. PRDX1-IN-3 also upregulates the downstream genes of the p53 signaling pathway to exert an anticancer effect .
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- HY-13757A
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Tamoxifen
Maximum Cited Publications
139 Publications Verification
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
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Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
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Endocrinology
Cancer
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Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .
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- HY-163378
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Complement System
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Inflammation/Immunology
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C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases .
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- HY-13757
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ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
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Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
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Cancer
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Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis . Tamoxifen Citrate also can induce gene knockout of CreER transgenic mouse .
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- HY-155539
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IKZF Family
Zinc Finger Protein
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Inflammation/Immunology
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Cisd2 agonist 2 (compound 6) is a Cisd2 activator (EC50=191 nM), and Cisd2 levels are associated with non-alcoholic fatty liver disease (NAFLD). Cisd2 agonist 2 has no significant in vivo toxicity in Cisd2hKO-het mice (heterozygous hepatocyte-specific Cisd2 knockout). Cisd2 (CDGSH iron sulfur domain 2) is a zinc finger protein that is mainly localized in the endoplasmic reticulum or mitochondrial membrane. Cisd2 participates in mitochondrial function by forming homodimers containing two redox-active 2Fe-2S clusters .
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- HY-168166
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Endogenous Metabolite
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Neurological Disease
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CHET3 is a sex-selective activator with potent analgesic activity. CHET3 was discovered to be a highly selective omnidirectional modulator of TASK-3-containing K2P channels, including TASK-3 homologues and TASK-3/TASK-1 heterologues. CHET3 exhibited significant analgesic effects in multiple acute and chronic pain models in mice, which could be abolished by pharmacological means or genetic knockout of TASK-3. CHET3 is able to functionally modulate the membrane excitability of specific small sensory neurons, which supports its analgesic effects on thermal hypersensitivity and mechanical hyperalgesia in chronic pain .
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- HY-13757AS1
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ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
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Cancer
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Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
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- HY-139289
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ART812
1 Publications Verification
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DNA/RNA Synthesis
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Cancer
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ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 has an IC50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ) .
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- HY-W778408
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ICI 47699-13C6; (Z)-Tamoxifen-13C6; trans-Tamoxifen-13C6
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Isotope-Labeled Compounds
Apoptosis
Autophagy
HSP
Estrogen Receptor/ERR
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Endocrinology
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Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .
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- HY-13757AR
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ICI 47699(Standard); (Z)-Tamoxifen(Standard); trans-Tamoxifen (Standard)
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Reference Standards
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
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Endocrinology
Cancer
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Tamoxifen (Standard) is the analytical standard of Tamoxifen (HY-13757A). This product is intended for research and analytical applications. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
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- HY-13757S
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ICI 46474-d3 hydrochloride; (Z)-Tamoxifen-d3 hydrochloride; trans-Tamoxifen-d3 hydrochloride
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Apoptosis
Estrogen Receptor/ERR
Autophagy
HSP
Isotope-Labeled Compounds
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Cancer
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Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
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- HY-115701
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1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-phosphoethanolamine; 15(S)-HpETE-SAPE; 15(S)-hydroperoxyeicostetraenoic acid-SAPE
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Ferroptosis
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Inflammation/Immunology
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1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-Pe is a phospholipid that contains stearic acid (HY-B2219) at the sn-1 position and 15(S)-HpETE at the sn-2 position. It is produced via oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-Pe (SAPE) by 15-lipoxygenase (15-LO). 1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-Pe (0.6 and 0.9 μM) increases ferroptotic cell death in wild-type and Acsl4 knockout Pfa1 mouse embryonic fibroblasts (MEFs) treated with the GPX4 inhibitor RSL3.
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- HY-126720
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Endogenous Metabolite
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Metabolic Disease
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N-Lignoceroyl Taurine is an arachidonoyl amino acid and taurine conjugate with a fatty acid that can be isolated from bovine brain. N-Lignoceroyl Taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of the brain and spinal cord of wild-type and fatty acid amide hydrolase (FAAH) knockout mice. N-Lignoceroyl Taurine levels were 23-26-fold higher in FAAH -/- mice compared to wild-type mice, suggesting that FAAH utilizes N-Lignoceroyl Taurine as a substrate. However, in vitro experiments with purified FAAH showed that N-Lignoceroyl Taurine was hydrolyzed 2,000-fold slower in FAAH compared to oleoylethanolamide. N-Acyl Taurines with polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) calcium channel family, including TRPV1 and TRPV4.
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- HY-13757R
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ICI 46474 (Standard); (Z)-Tamoxifen Citrate (Standard); trans-Tamoxifen Citrate (Standard)
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Reference Standards
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
Tamoxifen (Citrate) (Standard) is the analytical standard of Tamoxifen (Citrate). This product is intended for research and analytical applications. Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
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- HY-101563
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EPZ015938
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Histone Methyltransferase
SARS-CoV
MDM-2/p53
CDK
Apoptosis
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Infection
Cancer
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GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P5437
-
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PKC
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Others
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PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
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- HY-P10680
-
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Liposome
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Others
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TFE-IDAtp1-LinA is a highly potent amphiphilic carrier, containing a trifluoroethyl-iminodiacetic acid analog of Stp. TFE-IDAtp1-LinA, formed nanoparticles with Cas9 RNP/ssDNA, achieved enhanced green fluorescent protein knockouts with an ED50 of 0.38 nM Cas9/sgRNA ribonucleoproteins (RNP) .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-108786
-
ENB-0040
|
Phosphatase
|
Metabolic Disease
|
Asfotase alfa (ENB-0040) is a bone-targeted genetically engineered glycoprotein. Asfotase alfa increases the survival rate, bone mineralization and bone length and prevents mineralization defects of the feet, rib cage, lower limbs, jaw bones in Akp2 / knockout mice. Asfotase alfa can be used for the research of perinatal, infantile, and juvenile-onset hypophosphatasia (HPP) .
|
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- HY-P991477
-
|
CXCR
|
Inflammation/Immunology
|
HFB-100204 is a human monoclonal antibody (mAb) targeting CXCR5. HFB-100204 reduces CXCR5+ immune cells, including B cells and Tfh cells, in the blood and spleen of hCXCR5 knockout mice. HFB-100204 can be used in autoimmune diseases research .
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Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13757S
-
|
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
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- HY-13757AS1
-
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Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
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- HY-W778408
-
|
Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .
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Cat. No. |
Product Name |
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Classification |
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- HY-P10680
-
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Azide
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TFE-IDAtp1-LinA is a highly potent amphiphilic carrier, containing a trifluoroethyl-iminodiacetic acid analog of Stp. TFE-IDAtp1-LinA, formed nanoparticles with Cas9 RNP/ssDNA, achieved enhanced green fluorescent protein knockouts with an ED50 of 0.38 nM Cas9/sgRNA ribonucleoproteins (RNP) .
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