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constitutive

" in MedChemExpress (MCE) Product Catalog:

61

Inhibitors & Agonists

1

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1

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10

Peptides

1

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6

Natural
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3

Isotope-Labeled Compounds

6

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2

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-123051

    Proteasome Inflammation/Immunology
    Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate .
    Ac-WLA-AMC
  • HY-P10003B

    Proteasome Others
    iso-VQA-ACC acetate is a substrate for constitutive proteasome .
    iso-VQA-ACC acetate
  • 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-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-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-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-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-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-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-174717

    mRNA Cancer
    Human ERAS mRNA encodes the human ES cell expressed Ras (ERAS) protein, a constitutively active member of the small GTPase Ras protein family. ERAS may be involved in cancer and chemotherapy resistance.
    Human ERAS mRNA
  • 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-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-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-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-103243
    TCPOBOP
    3 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-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-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-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-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-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-N1943
    Ailanthone
    1 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-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-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-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-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-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)
  • 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-110134

    Constitutive Androstane Receptor Metabolic Disease
    S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC50 of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244) .
    S07662
  • HY-P2289A

    pBD-1 TFA

    Bacterial Infection
    β-defesin 1 (pig) (pBD-1) TFA is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites. β-defesin 1 (pig) TFA has antimicrobial activities and contributes to mucosal and systemic host defenses in pigs .
    β-defesin 1 (pig) (TFA)
  • HY-103243R

    Reference Standards Bcl-2 Family Cancer
    TCPOBOP (Standard) is the analytical standard of TCPOBOP. This product is intended for research and analytical applications. 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 (Standard)
  • 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-N7058

    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-134522

    Constitutive Androstane Receptor Metabolic Disease Cancer
    DL5050 is a selective and potent human constitutive androstane receptor (hCAR) agonist that does not activate pregnane X receptor (PXR). DL5050 preferentially induces the expression of CYP2B6 (target of hCAR) over CYP3A4 (target of hPXR) on both the mRNA and protein levels. DL5050 can be used for the researches of cancer and metabolic disease, such as diabetes .
    DL5050
  • HY-114180
    RU.521
    Maximum Cited Publications
    65 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-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-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-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-175167

    STING Inflammation/Immunology
    diABZI-i is a orthosteric STING inhibitor. diABZI-i significantly inhibits cGAMP-induced IFNβ in PBMCs with an IC50 of 49 nM. diABZI-i also activates V155M SAVI constitutive signaling in STING V155M THP-1 cells model with potent agonism (EC50: 17  nM). diABZI-i can be used for monogenic autoinflammatory disease like SAVI disease research .
    diABZI-i
  • HY-E70760

    Anaplastic lymphoma kinase (ALK) Cancer
    The NPM1-ALK protein contains the NPM1 oligomerization motif and the ALK catalytic domain, is constitutively activated through autophosphorylation, and mediates malignant cell transformation by activating downstream effectors including STAT3. NPM1 ALK Recombinant Human Active Protein Kinase is a recombinant NPM1 ALK protein that can be used to study NPM1 ALK-related functions .
    NPM1 ALK Recombinant Human Active Protein Kinase
  • HY-B0349B

    Meclozine dihydrochloride monohydrate

    Histamine Receptor Apoptosis Neurological Disease Inflammation/Immunology
    Meclizine (Meclozine) dihydrochloride monohydrate, 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 monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
    Meclizine dihydrochloride monohydrate
  • HY-B0349
    Meclizine dihydrochloride
    3 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-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-N7058S

    Isotope-Labeled Compounds Insecticide Others
    Cis-Jasmone-d2 is deuterated labeled Cis-Jasmone (HY-N7058). 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-d2
  • HY-E70761

    Anaplastic lymphoma kinase (ALK) Cancer
    The NPM1-ALK protein contains the NPM1 oligomerization motif and the ALK catalytic domain, is constitutively activated through autophosphorylation, and mediates malignant cell transformation by activating downstream effectors including STAT3. NPM1 ALK F1174L Recombinant Human Active Protein Kinase is a recombinant NPM1 ALK F1174L protein that can be used to study NPM1 ALK F1174L-related functions .
    NPM1 ALK F1174L Recombinant Human Active Protein Kinase
  • HY-19989
    MK-571
    25+ 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-16697R

    GPR55 Cancer
    CID 16020046 (Standard) is the analytical standard of CID 16020046. This product is intended for research and analytical applications. 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 Ca2+ 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 (Standard)
  • 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-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

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