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knockout

" in MedChemExpress (MCE) Product Catalog:

30

Inhibitors & Agonists

1

Peptides

1

Inhibitory Antibodies

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W747072
    3-Sulfo-taurocholic Acid Disodium Salt

    3-Sulfocholyl Taurine; TCA3S

    		 Others Metabolic Disease
    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.
    3-Sulfo-taurocholic Acid Disodium Salt
  • HY-136057
    iFSP1
    10+ Cited Publications

    		 Ferroptosis Cancer
    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) .
    iFSP1
  • HY-160887
    FPT

    		5-HT Receptor Neurological Disease
    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 .
    FPT
  • HY-19914
    MK-1064
    2 Publications Verification

    		 Orexin Receptor (OX Receptor) Endocrinology Cancer
    MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia .
    MK-1064
  • HY-161246
    uPSEM792

    		Others Neurological Disease
    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 .
    uPSEM792
  • HY-148764
    M47

    		Apoptosis Cancer
    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 .
    M47
  • HY-P5437
    PKCε (85-92)

    		PKC Others
    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.)
    PKCε (85-92)
  • HY-161671
    GAT2711

    		nAChR Neurological Disease
    GAT2711 (compound 3h) is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells and exhibits analgesic activity in α7 knockout mice .
    GAT2711
  • HY-149611
    Lysyl hydroxylase 2-IN-2

    		Monoamine Oxidase Cancer
    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 .
    Lysyl hydroxylase 2-IN-2
  • HY-117764
    LSP4-2022

    		mGluR Neurological Disease
    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 .
    LSP4-2022
  • HY-111287
    Autophagonizer

    DK-1-49

    		 Autophagy Cancer
    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 .
    Autophagonizer
  • HY-155539
    Cisd2 agonist 2
    1 Publications Verification

    		 Others Inflammation/Immunology
    Cisd2 agonist 2 (compound 6) is an orally active Cisd2 activator (EC50=191 nM), while the Cisd2 levels is correlated with nonalcoholic fatty liver disease (NAFLD). Cisd2 agonist 2 has no significant toxicity in vivo in Cisd2hKO-het mice (heterozygous hepatocyte-specific Cisd2 knockout) .
    Cisd2 agonist 2
  • HY-103259
    Sodium metatungstate
    5+ Cited Publications

    Sodium polyoxotungstate; POM-1

    		 Phosphatase P2X Receptor P2Y Receptor Pyroptosis Interleukin Related Neurological Disease Inflammation/Immunology Cancer
    Sodium metatungstate (Sodium polyoxotungstate) is a NTPDase inhibitor, with Ki values of 2.58 μM, 3.26 μM, and 28.8 μM for NTPDase 1 (CD39), NTPDase 3 and NTPDase 2 respectively . Sodium metatungstate has anti-inflammatory and anti-cancer effect. Sodium metatungstate inhibits ATP breakdown but also blocks central synaptic transmission .
    Sodium metatungstate
  • HY-103259A
    Sodium metatungstate hydrate

    Sodium polyoxotungstate hydrate; POM-1 hydrate

    		 NTPDase Pyroptosis Neurological Disease Inflammation/Immunology Cancer
    Sodium metatungstate (Sodium polyoxotungstate; POM-1) hydrate is a NTPDase inhibitor, with Ki values of 2.58 μM, 3.26 μM, and 28.8 μM for NTPDase 1 (CD39), NTPDase 3 and NTPDase 2 respectively . Sodium metatungstate has anti-inflammatory and anti-cancer effect. Sodium metatungstate inhibits ATP breakdown but also blocks central synaptic transmission .
    Sodium metatungstate hydrate
  • HY-16968
    SW033291
    5+ Cited Publications

    		 15-PGDH Others
    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 .
    SW033291
  • HY-154979
    Anti-hepatic fibrosis agent 2

    		Others Inflammation/Immunology
    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) .
    Anti-hepatic fibrosis agent 2
  • HY-135555
    5-Carboxamidotryptamine

    5-CT

    		 5-HT Receptor Neurological Disease
    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 .
    5-Carboxamidotryptamine
  • HY-13757A
    Tamoxifen
    Maximum Cited Publications
    111 Publications Verification

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    		 Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    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 .
    Tamoxifen
  • HY-163378
    C5aR1 antagonist 1

    		Complement System Inflammation/Immunology
    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 .
    C5aR1 antagonist 1
  • HY-168166
    CHET3

    		Others Neurological Disease
    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 .
    CHET3
  • HY-13757
    Tamoxifen Citrate
    Maximum Cited Publications
    111 Publications Verification

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    		 Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    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 .
    Tamoxifen Citrate
  • HY-139289
    ART812
    1 Publications Verification

    		 DNA/RNA Synthesis Cancer
    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) .
    ART812
  • HY-13757AS1
    Tamoxifen-d3

    ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3

    		 Estrogen Receptor/ERR Apoptosis Autophagy HSP Cancer
    Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. 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[2][3][4]. 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[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
    Tamoxifen-d3
  • HY-13757AR
    Tamoxifen (Standard)
    100+ Cited Publications

    ICI 47699(Standard); (Z)-Tamoxifen(Standard); trans-Tamoxifen (Standard)

    		 Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen (Standard) is the analytical standard of Tamoxifen. 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 .
    Tamoxifen (Standard)
  • HY-13757S
    Tamoxifen-d3 hydrochloride

    ICI 46474-d3 hydrochloride; (Z)-Tamoxifen-d3 hydrochloride; trans-Tamoxifen-d3 hydrochloride

    		 Apoptosis Estrogen Receptor/ERR Autophagy HSP Isotope-Labeled Compounds Cancer
    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 .
    Tamoxifen-d3 hydrochloride
  • HY-126720
    N-Lignoceroyl Taurine

    		Endogenous Metabolite Metabolic Disease
    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.
    N-Lignoceroyl Taurine
  • HY-115701
    1-Stearoyl-2-15(S)-Hpete-Sn-Glycero-3-Pe

    1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-phosphoethanolamine; 15(S)-HpETE-SAPE; 15(S)-hydroperoxyeicostetraenoic acid-SAPE

    		 Others Inflammation/Immunology
    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.
    1-Stearoyl-2-15(S)-Hpete-Sn-Glycero-3-Pe
  • HY-13757R
    Tamoxifen Citrate (Standard)

    		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 .
    Tamoxifen Citrate (Standard)
  • HY-101563
    GSK3326595
    15+ Cited Publications

    EPZ015938

    		 Histone Methyltransferase SARS-CoV MDM-2/p53 CDK Apoptosis Infection Cancer
    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 .
    GSK3326595
  • HY-117051
    STA-2842

    		Others Cancer
    STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
    STA-2842

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