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Results for "

constitutive

" in MedChemExpress (MCE) Product Catalog:

87

Inhibitors & Agonists

1

Screening Libraries

1

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11

Peptides

2

Inhibitory Antibodies

7

Natural
Products

1

Recombinant Proteins

3

Isotope-Labeled Compounds

8

Antibodies

3

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114180
    RU.521
    Maximum Cited Publications
    83 Publications Verification

    RU320521

    Cyclic GMP-AMP Synthase Metabolic Disease
    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS) .
    RU.521
  • HY-19989
    MK-571
    30+ Cited Publications

    L-660711

    P-glycoprotein LPL Receptor Leukotriene Receptor Inflammation/Immunology
    MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
    MK-571
  • HY-19989A
    MK-571 sodium
    30+ Cited Publications

    L-660711 sodium

    P-glycoprotein LPL Receptor Leukotriene Receptor Inflammation/Immunology
    MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
    MK-571 sodium
  • HY-103244
    CITCO
    3 Publications Verification

    Apoptosis Cancer
    CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors .
    CITCO
  • HY-138188
    KRA-533
    1 Publications Verification

    Ras Cancer
    KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
    KRA-533
  • HY-103243
    TCPOBOP
    4 Publications Verification

    Bcl-2 Family Cancer
    TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss . TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins .
    TCPOBOP
  • HY-N1943
    Ailanthone
    2 Publications Verification

    Δ13-Dehydrochaparrinone

    Androgen Receptor Inflammation/Immunology Cancer
    Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
    Ailanthone
  • HY-B0349
    Meclizine dihydrochloride
    4 Publications Verification

    Meclozine dihydrochloride

    Histamine Receptor Apoptosis Neurological Disease Endocrinology Cancer
    Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
    Meclizine dihydrochloride
  • HY-16697
    CID 16020046
    2 Publications Verification

    GPR55 Cancer
    CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
    CID 16020046
  • HY-W140439

    18:1 Lyso PC

    Endogenous Metabolite Inflammation/Immunology
    1-Oleoyl-sn-glycero-3-phosphocholine (18:1 Lyso PC), a lysophospholipid, is a GPR82 inhibitor. 1-Oleoyl-sn-glycero-3-phosphocholine abrogates constitutive Gi-coupled GPR82 activity, shifts active/inactive equilibrium to inactive, suppresses Gi protein activation, increases cAMP production, and decreases GTPγS binding to Gαi proteins. 1-Oleoyl-sn-glycero-3-phosphocholine contributes to adipocyte lipolysis regulation.1-Oleoyl-sn-glycero-3-phosphocholine exhibits reduced serum levels in mouse models of steatohepatitis, linked to hepatic Lpcat 1-4 up-regulation .
    1-Oleoyl-sn-glycero-3-phosphocholine
  • HY-P11307

    Proteasome Cancer
    Biotin-epoxomicin is a Proteasome subunit binder. Biotin-epoxomicin serves as an affinity reagent for identifying proteasomal catalytic subunits, and facilitates affinity purification of active proteasomal subunits for LC-MS identification. Biotin-epoxomicin can be used to study solid tumors derived from B16 melanoma .
    Biotin-epoxomicin
  • HY-P991558

    RG-7356

    Transmembrane Glycoprotein Cancer
    RO-5429083 (RG-7356) is a humanized monoclonal antibody targeting CD44. RO-5429083 binds to the extracellular domain of CD44 and inhibits constitutive EGFR phosphorylation. RO-5429083 suppresses tumor growth in xenograft models and can be used in research related to head and neck squamous cell carcinoma and acute myeloid leukemia .
    RO-5429083
  • HY-P99419

    GEN1046

    PD-1/PD-L1 Cancer
    Acasunlimab (GEN1046) is a bispecific antibody (bsAb) targeting PD-L1 and 4-1BB. Acasunlimab enhances T-cell and NK-cell function through conditional 4-1BB stimulation while constitutively blocking the PD-1/PD-L1 inhibitory axis. Acasunlimab can be used in research of cancer .
    Acasunlimab
  • HY-15446
    Basimglurant
    1 Publications Verification

    RG7090; RO4917523

    mGluR Neurological Disease
    Basimglurant (RG7090; RO4917523) is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a Ki of 1.4 nM (against [ 3H]-ABP688 (HY-110141)) and 35.6 nM (against [ 3H]-MPEP (HY-14609A)). Basimglurant inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant can be used in research on depression, fragile X syndrome, anxiety disorders, etc .
    Basimglurant
  • HY-N7058

    Environmental Pollutants Insecticide Others
    Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies .
    cis-​Jasmone
  • HY-15873A

    Farnesyl Transferase Ras p38 MAPK Cancer
    FTI 276 TFA is a farnesyltransferase (FTase) inhibitor with an IC50 of 0.5 nM, and it exhibits selectivity for FTase over geranylgeranyltransferase I (GGTase I). FTI 276 TFA blocks the farnesylation of H-Ras and K-Ras4B, causes inactive Ras-Raf complexes to accumulate in the cytoplasm, and inhibits constitutive MAPK activation. FTI 276 TFA reduces the number, incidence and volume of tumors, and restricts the growth of tumors expressing activated K-ras. FTI 276 TFA can be used in research related to pulmonary adenoma .
    FTI 276 TFA
  • HY-112338

    CPD188

    STAT Apoptosis Cancer
    C188 (CPD188) is a STAT3 inhibitor with anticancer effects. C188 inhibits STAT3 SH2/pY-peptide binding (IC50 of 20 µM against pY-peptide binding) and IL-6-mediated STAT3 phosphorylation. C188 is selective for STAT3 over STAT1. C188 inhibits nuclear-to-cytoplasmic translocation of Stat3. C188 shows highly active induces apoptosis in breast cancer cell lines with constitutive Stat3 activation (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively) .
    C188
  • HY-123051

    Proteasome Inflammation/Immunology
    Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .
    Ac-WLA-AMC
  • HY-W013854

    3β-Hydroxy-5α-androstane

    Endogenous Metabolite Others
    5α-Androstan-3β-ol (Androstan), a saturated sterol, is a CAR (constitutive androstane receptor) inverse agonist ligand. 5α-Androstan-3β-ol (Androstan) increases the AmB-channel conductance in a concentration dependent manner .
    5α-Androstan-3β-ol
  • HY-120210

    ROR Inflammation/Immunology Cancer
    XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .
    XY018
  • HY-110249
    CINPA1
    1 Publications Verification

    Constitutive Androstane Receptor Metabolic Disease
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .
    CINPA1
  • HY-N8146

    STAT Bcl-2 Family Ser/Thr Kinase Survivin c-Myc Apoptosis Necroptosis CDK Infection Cancer
    Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
    Bruceantinol
  • HY-P10115

    STAT Cancer
    APT STAT3 is a specific STAT3-binding peptide. APT STAT3 can bind STAT3 with high specificity and affinity (~231 nmol/L). APT STAT3 is a tractable agent for translation to target the broad array of cancers harboring constitutively activated STAT3 .
    APT STAT3
  • HY-175167

    STING IFNAR Inflammation/Immunology
    diABZI-i is an orthogonal STING inhibitor. diABZI-i significantly inhibits cGAMP-induced IFNβ in PBMCs. diABZI-i also activates constitutive signaling of V155M SAVI and exerts potent agonistic effects in the STING V155M THP-1 cell model. diABZI-i can be used for research on monogenic autoinflammatory diseases such as SAVI .
    diABZI-i
  • HY-136748
    HIF-2α-IN-4
    1 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing .
    HIF-2α-IN-4
  • HY-P0271A
    Syntide 2 TFA
    2 Publications Verification

    CaMK Neurological Disease
    Syntide 2 (TFA), a Ca 2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected .
    Syntide 2 TFA
  • HY-174631

    mRNA Inflammation/Immunology
    Human IL18 mRNA encodes the human interleukin 18 (IL18) protein, a proinflammatory cytokine of the IL-1 family. IL18 is constitutively found as a precursor within the cytoplasm of a variety of cells including macrophages and keratinocytes. This cytokine has been implicated in the injury of different organs, and in potentially fatal conditions characterized by a cytokine storm.
    Human IL18 mRNA
  • HY-P10003B

    Proteasome Others
    iso-VQA-ACC acetate is a substrate for constitutive proteasome .
    iso-VQA-ACC acetate
  • HY-18952A

    FLT3 Apoptosis Cancer
    (Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3 .
    (Z)-SU5614
  • HY-B0349A

    Meclozine

    Histamine Receptor Apoptosis Neurological Disease Inflammation/Immunology
    Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
    Meclizine
  • HY-N7058R

    Reference Standards Insecticide Others
    cis-Jasmone (Standard) is the analytical standard of cis-Jasmone. This product is intended for research and analytical applications. Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies .
    cis-?Jasmone (Standard)
  • HY-170881

    Proteasome Cancer
    TIR-199 is a novel and highly specific dual proteasome inhibitor that can effectively inhibit the PSMB5 subunit of constitutive proteasome and the PSMB8 subunit of immunoproteasome. TIR-199 can induce the death of various tumor cells. TIR-199 can be used for research on myeloma .
    TIR-199
  • HY-153095

    GHSR Metabolic Disease
    PF-6870961 is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM .
    PF-6870961
  • HY-111634

    Constitutive Androstane Receptor Cancer
    Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats .
    Epsilon-momfluorothrin
  • HY-173465

    Constitutive Androstane Receptor Metabolic Disease Cancer
    DL5055 (compound 6k) is a potent and selective hCAR activator with an EC50 of 0.35 μM. DL5055 induces CYP2B6 expression and hCAR nuclear translocation in human primary hepatocytes .
    DL5055
  • HY-P0271

    CaMK Autophagy Neurological Disease
    Syntide 2, a Ca 2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected .
    Syntide 2
  • HY-128762

    Phospholipase Cancer
    ML256 is a covalent lipoprotein-associated phospholipase A2 (Lp-PLA2 inhibitor. ML256 can be used for the study of neoplasms harboring a constitutively active variant of one or both of KRAS or HRAS .
    ML256
  • HY-124605

    Syk Btk Apoptosis Cancer
    IQS-019 is a B cell receptor (BCR) kinase inhibitor. IQS-019 can inhibit the de-phosphorylation of constitutive and IgM-activated Syk, Lyn, and Btk. IQS-019 can inhibit cell proliferation, migration and induce apoptosis. IQS-019 exhibits antitumor activity and can be used for the research of cancer, such as B cell lymphoma .
    IQS-019
  • HY-W722556

    3α,5α-Androstanol

    GABA Receptor Constitutive Androstane Receptor Metabolic Disease
    5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms .
    5α-Androstan-3α-ol
  • HY-173033

    Pregnane X Receptor (PXR) Constitutive Androstane Receptor Cytochrome P450 Metabolic Disease
    MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC50=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC50=0.1 μM). MI-883 stimulates CAR LBD assembly (EC50=0.38 µM) and CAR3 variant activation (EC50=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC50=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .
    MI-883
  • HY-P10003

    Proteasome Cancer
    iso-VQA-ACC is a substrate for constitutive proteasome .
    iso-VQA-ACC
  • HY-P10003A

    Proteasome Others
    iso-VQA-ACC TFA is a constitutive proteasome substrate .
    iso-VQA-ACC TFA
  • HY-153095A

    GHSR Metabolic Disease
    PF-6870961 hydrochloride is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 hydrochloride inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 hydrochloride also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM .
    PF-6870961 hydrochloride
  • HY-155295

    Constitutive Androstane Receptor Drug Isomer Metabolic Disease
    Z-CITCO is the cis isomer of CITCO (HY-103244). Z-CITCO is an agonist of constitutive androstane receptor (CAR) with an EC50 value of 3.9 µM .
    Z-CITCO
  • HY-U00432B

    S-Methyl-L-thiocitrulline acetate

    NO Synthase Endogenous Metabolite Inflammation/Immunology
    S-MTC acetate (S-Methyl-L-thiocitrulline acetate) acts as a powerful inhibitor of inducible nitric oxide synthase, favoring the inhibition of constitutive (neuronal) nitric oxide synthase over inducible (endothelial) nitric oxide synthase.
    S-MTC acetate
  • HY-147563

    RET Cancer
    RET-IN-17 is a potent inhibitor of RET. RET-IN-17 has the potential for the research of pain associated with IBS and other gastrointestinal disorders and for the research of cancers with constitutive RET kinase activity (extracted from patent WO2016038552A1, compound 1) .
    RET-IN-17
  • HY-103289

    Bradykinin Receptor Metabolic Disease Inflammation/Immunology
    MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with a pKi value of 10.3 .
    MEN 11270
  • HY-B0349S

    Meclozine-d8

    Isotope-Labeled Compounds Histamine Receptor Apoptosis Inflammation/Immunology
    Meclizine-d8 is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
    Meclizine-d8
  • HY-161980

    Topoisomerase Infection
    Topoisomerases/ribosomes-IN-1 (compound 30f) is an inhibitor of ribosomes and topoisomerases, and has inhibitory effects on constitutively macrolide-resistant bacteria. Topoisomerases/ribosomes-IN-1 can inhibit bacterial protein synthesis (IC50: 0.647 μM) and DNA replication (IC50: 0.218 μM) .
    Topoisomerases/ribosomes-IN-1
  • HY-P2289

    pBD-1

    Bacterial Infection
    β-defesin 1 (pig) (pBD-1) is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites. β-defesin 1 (pig) has antimicrobial activities and contributes to mucosal and systemic host defenses in pigs .
    β-defesin 1 (pig)

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