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Activators and Inhibitors

" in MedChemExpress (MCE) Product Catalog:

2941

Inhibitors & Agonists

17

Screening Libraries

14

Fluorescent Dye

25

Biochemical Assay Reagents

183

Peptides

44

Inhibitory Antibodies

629

Natural
Products

192

Isotope-Labeled Compounds

4

Click Chemistry

17

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0277
    Aconine
    2 Publications Verification

    Jesaconine

    NF-κB Inflammation/Immunology Cancer
    Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.
    Aconine
  • HY-107753

    Ras Inflammation/Immunology Cancer
    XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2 . XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules .
    XRP44X
  • HY-130480

    AIM2 Inflammation/Immunology
    Fructose-arginine, an amino-sugar, is an AIM2 inflammasome activation inhibitor. Fructose-arginine attenuates the secretion of IL-1β, IL-18, and caspase-1, and Asc pyroptosome formation and Gsdmd cleavage resulting from AIM2 inflammasome activation .
    Fructose-arginine
  • HY-142163

    Thrombin Cardiovascular Disease
    S62798 is a selective and potent inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) with an IC50 value of 6 mM.
    S62798
  • HY-176427

    ClpP Cancer
    HsClpP activator-1 (compound 24) is a potent HsClpP activator with an EC50 of 0.22 μM. HsClpP activator-1 effectively inhibits cancer cell growth with IC50 values of 0.1-1 μM .
    HsClpP activator-1
  • HY-156081

    Keap1-Nrf2 Apoptosis Metabolic Disease
    Nrf2 activator-9 (compound D-36) is an Nrf2 activator that inhibits oxidized low-density lipoprotein (oxLDL) and high glucose (HG)-induced apoptosis in HUVEC cells. Nrf2 activator-9 inhibits oxLDL and HG-induced vascular endothelial cell (VEC) injury and can effectively prevent and treat atherosclerosis .
    Nrf2 activator-9
  • HY-148480

    Quinone Reductase Keap1-Nrf2 Cardiovascular Disease
    Nrf2 activator-6, a tetrahydroisoquinoline compound, is a Nrf2 activator. Nrf2 activator-6 has an IC50 of 5 nM for inhibiting the Kelch domain-Nrf2 interaction (WO2021214470A1; Example 4) .
    Nrf2 activator-6
  • HY-N10782

    Apoptosis COX TNF Receptor p38 MAPK Neurological Disease Inflammation/Immunology Cancer
    Balanophonin is an anti-inflammatory and anti-cancer agent. Balanophonin inhibits microglial activation and neurodegeneration via inhibiting activated microglia-induced apoptosis .
    Balanophonin
  • HY-172596

    JAK Inflammation/Immunology
    TYK2 activator-1 (16b) is a TYK2 activator with anEC50 of 1.78 μM. TYK2 activator-1 inhibits JAK2 and JAK3 with the IC50 values of 6.8 and 6.3 μM, respectively .
    TYK2 activator-1
  • HY-156375

    Pyruvate Kinase PDK-1 Cancer
    PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM) .
    PKM2 activator 6
  • HY-14754
    Salirasib
    5+ Cited Publications

    S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS

    Ras Autophagy Cancer
    Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
    Salirasib
  • HY-170918

    Potassium Channel Others
    BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC50 of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model .
    BKCa activator-1
  • HY-173399

    STING Interleukin Related IFNAR Inflammation/Immunology Cancer
    hSTING activator-1 (Compound 68) is a STING agonist. hSTING activator-1 can effectively activate multiple human STING variants (R232, H232, HAQ) with EC50 values of 56 nM, 89 nM and 51 nM, respectively. hSTING activator-1 activates the type I interferon pathway by directly binding to STING protein and stabilizing its conformation, promoting downstream IRF3 phosphorylation and cytokine release. hSTING activator-1 inhibits fibrosarcoma tumor growth and has potential in cancer research .
    hSTING activator-1
  • HY-113817

    Phosphatase Inflammation/Immunology
    SHIP1 activator 1 is an SH3 domain-containing inositol 5-phosphatase regulator with SHIP1 activating activity. SHIP1 activator 1 retains its SHIA-1 activating ability by removing unnecessary functional groups. SHIP1 activator 1 is able to activate SHIP1 in vitro, inhibit Akt phosphorylation in MOLT-4 cells, and show dose-dependent activity in a mouse model of inflammation. SHIP1 activator 1 is an important chemical tool for evaluating the potential of SHIP1 activators as inhibitors of hematopoietic diseases involving abnormal PI3K cell signaling .
    SHIP1 activator 1
  • HY-114304
    COH000
    1 Publications Verification

    E1/E2/E3 Enzyme Cancer
    COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro .
    COH000
  • HY-155363

    AMPK Metabolic Disease
    AMPK activator 13 is a potent activator of AMPK. AMPK activator 13 inhibits mitotic clonal expansion of 3T3-L1 cells by activating AMPK pathway and enhances cell mitochondrial oxygen consumption rate. AMPK activator 13 can be used in study obesity .
    AMPK activator 13
  • HY-154973

    Oxidative Phosphorylation Mitochondrial Metabolism AMPK Metabolic Disease Cancer
    AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research .
    AMPK activator 11
  • HY-124445

    NF-κB Inflammation/Immunology
    APC0576 is an inhibitor for the activation of NF-κB signaling pathway, and inhibits the activation of NF-κB depedent gene (IC50 is 1.0 μM for β-gal). APC0576 inhibits IL-1-induced chemokines release, and can be used in research about pathological endothelial cell activation releted diseases .
    APC0576
  • HY-145879

    Keap1-Nrf2 Cancer
    Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells .
    Nrf2 activator-2
  • HY-19635A
    G-5555 hydrochloride
    5+ Cited Publications

    PAK Cancer
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
    G-5555 hydrochloride
  • HY-135825
    TFEB activator 1
    5 Publications Verification

    Autophagy Neurological Disease
    TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment .
    TFEB activator 1
  • HY-N4231

    NF-κB Inflammation/Immunology
    Lucyoside B inhibits the production of inflammatory mediators via both NF-κB and activator protein-1 pathways in activated macrophages .
    Lucyoside B
  • HY-15723A
    NSC 23766 trihydrochloride
    35+ Cited Publications

    Ras Apoptosis Cancer
    NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.
    NSC 23766 trihydrochloride
  • HY-161929

    Glutathione Peroxidase Ferroptosis Cardiovascular Disease
    GPX4 activator 2 (Compound C3) is an activator of GPX4. GPX4 activator 2 exhibits cardioprotective effects and can inhibit cellular ferroptosis (EC50=7.8 μM). GPX4 activator 2 can be used in the research of myocardial injury .
    GPX4 activator 2
  • HY-170591

    MDM-2/p53 Apoptosis Cancer
    p53 Activator 14 (Compound 7A) is a derivative of Neratinib (HY-32721), that induces DNA damage, activates p53, and inhibits the proliferation of multi cancer cells (IC50=7.21 μM for HCT116 cell). p53 Activator 14 inhibits the adhesion, migration and invasion of HCT116, arrests the cell cycle, and induces apoptosis. p53 Activator 14 inhibits angiogenesis and exhibits antitumor efficacy in chick chorioallantoic membrane (CAM) model .
    p53 Activator 14
  • HY-176426

    Deubiquitinase NF-κB IFNAR Cancer
    Subquinocin is a CYLD inhibitor that inhibits USP family deubiquitinases (DUBs). Subquinocin enhances the activation of NF-κB and IFN pathways by inhibiting CYLD. Subquinocin promotes RIG-I-mediated activation of IRF3 and/or IRF7 in the interferon pathway .
    Subquinocin
  • HY-101796

    Ras SOS1 Cancer
    NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect .
    NSC-70220
  • HY-121896

    SHP2 Cancer
    DSHN is a potent small heterodimer partner (SHP) activator. DSHN inhibits Ccl2 expression and secretion by inhibiting p65 activation of Ccl2 promoter activity. DSHN can be used in research of cancer .
    DSHN
  • HY-118792

    Endogenous Metabolite Cancer
    AHR activator 1 is an aryl hydrocarbon receptor activator with activity regulating fibroblast growth factor-2 (FGF2)-induced branching morphogenesis. AHR activator 1 prevents the formation of cellular branches by inhibiting AHR signaling. AHR activator 1 also associates with adhesion of dissociated linkers, suggesting the importance of dissociated linkers in the inhibition of branching by AHR agonists. Studies of AHR activator 1 reveal its functional role in mammary gland morphogenesis and play a role in inhibiting FGF-induced invasion .
    AHR activator 1
  • HY-131521

    Oxalomalate trisodium

    Isocitrate Dehydrogenase (IDH) Cancer
    Oxalomalic acid (Oxalomalate) trisodium is a aconitase and NADP-dependent isocitrate dehydrogenase inhibitor. Oxalomalic acid trisodium inhibits nitrite production and iNOS protein expression in lipopolysaccharide (HY-D1056)-activated J774 macrophages .
    Oxalomalic acid trisodium
  • HY-100472

    Caspase Cancer
    ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3 .
    ZYZ-488
  • HY-173307

    Keap1-Nrf2 Apoptosis Reactive Oxygen Species (ROS) Cardiovascular Disease
    Nrf2 activator 19 is a BBB-penetrable NRF2/HO-1 activator. Nrf2 activator 19 exerts potent antioxidant and neuroprotective effects. Nrf2 activator 19 can also effectively reduce brain damage, reduce Reactive Oxygen Species (ROS) accumulation. Nrf2 activator 19 inhibits neuronal apoptosis. Nrf2 activator 19 promotes the recovery of neurological function and motor ability. Nrf2 activator 19 shows significant potential in ischemic stroke research .
    Nrf2 activator 19
  • HY-P1376

    mAChR Adrenergic Receptor Endocrinology
    G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
    G-Protein antagonist peptide
  • HY-N10458

    NF-κB Inflammation/Immunology
    Asperbisabolane L, a sesquiterpenoid, exerts the anti-inflammatory activity by inhibiting the NF-κB-activated pathway. Asperbisabolane L inhibits the translocation of NF-κB from cytoplasm to the nucleus. Asperbisabolane L also inhibits NO production in LPS-activated BV-2 microglia cells .
    Asperbisabolane L
  • HY-172901

    AMPK Cardiovascular Disease Metabolic Disease
    AMPK activator 17 (Compound 10g) is an orally active AMPK activator. AMPK activator 17 has significant anti-adipogenic (IC50: 3.4 μM) and dyslipidemia-modifying activities. AMPK activator 17 inhibits the early stages of adipocyte differentiation (mitotic clonal expansion) by activating the AMPK pathway. AMPK activator 17 can enhance mitochondrial function and fatty acid oxidation in mature adipocytes. AMPK activator 17 improves dyslipidemia by promoting reverse cholesterol transport. AMPK activator 17 can be used in the study of obesity and related metabolic diseases (such as type 2 diabetes and cardiovascular disease) .
    AMPK activator 17
  • HY-168636

    DNA Methyltransferase MDM-2/p53 Cancer
    p53 Activator 13 (compound 11) is a 6mA methyltransferase CamA inhibitor and a p53 activator. p53 Activator 13 intercalates into CamA-bound DNA via the minor groove, causing a conformational shift that moves the catalytic domain away from the DNA and elicits DNA damage response via p53 activation. p53 Activator 13 can be utilized in cancer research .
    p53 Activator 13
  • HY-15542A
    FRAX597
    5+ Cited Publications

    PAK Cancer
    FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
    FRAX597
  • HY-P1918
    Activated Protein C (390-404), human
    4 Publications Verification

    Ser/Thr Protease Cardiovascular Disease
    Activated Protein C (390-404), human is a peptide of the activated protein C (a vitamin K-dependent serine protease), potently inhibits APC anticoagulant activity .
    Activated Protein C (390-404), human
  • HY-15870
    SR 11302
    5+ Cited Publications

    AP-1 Inflammation/Immunology Cancer
    SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE) .
    SR 11302
  • HY-W006230

    Cytochrome P450 Cancer
    Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens .
    Anthraflavic acid
  • HY-14452
    Fatostatin
    30+ Cited Publications

    125B11

    Fatty Acid Synthase (FASN) Cancer
    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice .
    Fatostatin
  • HY-169315

    Keap1-Nrf2 Cancer
    Nrf2 activator 17 (compound 10) is an Nrf2 activator that inhibits the interaction between Keap1 and Nrf2 with an IC50 of < 0.1 pM. Additionally, Nrf2 activator 17 has an EC50 of < 10 μM in HepG2 cells .
    Nrf2 activator 17
  • HY-168640

    Autophagy Necroptosis RIP kinase Cancer
    RIP3 activator 1 (compound C8) is a potent RIP3 activator. RIP3 activator 1 inhibits cell growth. RIP3 activator 1 induces necroptosis through the RIP3/p62/Keap1 signaling pathway. RIP3 activator 1 increases the protein expression of p-MLKL. RIP3 activator 1 induces autophagy. RIP3 activator 1 increases accumulation of LC3-II and p62 protein expression .
    RIP3 activator 1
  • HY-170931

    AMPK Acetyl-CoA Carboxylase Neurological Disease Metabolic Disease
    AMPK activator 16 (compound 6) is a AMP-activated protein kinase (AMPK) inhibitor. AMPK activator 16 shows the most efficient interactions with the key residues of AMPK and demonstrates significant activation of AMPK. AMPK activator 16 increases the expression of phosphorylated AMPK (p-AMPK) and its downstream signaling proteins, such as phosphorylated ACC (Acetyl-CoA Carboxylase) (p-ACC) and phosphorylated raptor (p-raptor), in N2a cells .
    AMPK activator 16
  • HY-N6688

    Potassium Channel Bacterial Antibiotic Infection
    Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle .
    Verruculogen
  • HY-15027
    5-Aminosalicylic Acid
    15+ Cited Publications

    Mesalamine; 5-ASA; Mesalazine

    PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
    5-Aminosalicylic Acid
  • HY-P1918A

    APC Cardiovascular Disease
    Activated Protein C (390-404), human TFA, a peptide of the activated protein C (a vitamin K-dependent serine protease), potently inhibits APC anticoagulant activity .
    Activated Protein C (390-404), human TFA
  • HY-110105

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively) .
    NS8593 hydrochloride
  • HY-101918

    Thrombin Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases .
    DS-1040 Tosylate
  • HY-14754R

    S-Farnesylthiosalicylic acid (Standard); Farnesyl Thiosalicylic Acid (Standard); FTS (Standard)

    Reference Standards Ras Autophagy Cancer
    Salirasib (Standard) is the analytical standard of Salirasib. This product is intended for research and analytical applications. Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
    Salirasib (Standard)