1. Search Result
Search Result
Results for "

allosteric activation

" in MedChemExpress (MCE) Product Catalog:

148

Inhibitors & Agonists

1

Biochemical Assay Reagents

7

Peptides

10

Natural
Products

7

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-139303

    GnRH Receptor Endocrinology
    LUF5771 is a potent allosteric recombinant luteinizing hormone (recLH) and Org 43553 inhibitor. LUF5771 is able to partially activate the LH receptor with low efficacy .
    LUF5771
  • HY-161296

    Bacterial HIV Infection
    TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe .
    TH6342
  • HY-B1456A
    Fenoprofen
    1 Publications Verification

    LILLY-53858

    COX Melanocortin Receptor ERK Inflammation/Immunology
    Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
    Fenoprofen
  • HY-101796

    Ras 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-59047
    Tolimidone
    4 Publications Verification

    MLR-1023

    Src Metabolic Disease
    Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.
    Tolimidone
  • HY-110087

    nAChR Neurological Disease
    4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site .
    4BP-TQS
  • 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-171177

    Phosphatase Neurological Disease Cancer
    P5SA-2 is a selective allosteric activator of PPP5C. P5SA-2 exerts its effects by modulating the phosphatase domain of PPP5C and can increase PPP5C activity by 3.2-fold at 100 μM with an apparent affinity constant of 7.8 μM. P5SA-2 can be used in cancer and Alzheimer's disease research .
    P5SA-2
  • HY-B1456AR

    LILLY-53858 (Standard)

    COX Melanocortin Receptor ERK Inflammation/Immunology
    Fenoprofen (Standard) (LILLY-53858 (Standard)) is the analytical standard of Fenoprofen (HY-B1456A). This product is intended for research and analytical applications. Fenoprofenc is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
    Fenoprofen (Standard)
  • HY-130155

    AMPK Neurological Disease
    AMPK activator C2 is a potent allosteric AMPK activator that is promising for research of epilepsy and convulsions .
    AMPK activator C2
  • HY-157421

    NAMPT Others
    Nampt activator-4 is a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of 0.058 μM. Nampt activator-4 can enhance the nicotinamide adenine dinucleotide (NAD +) in cells .
    Nampt activator-4
  • HY-173352

    Deubiquitinase Cancer
    USP7 activator 1 (compound MS-8) is an activator of USP7 by engaging the allosteric C-terminal binding pocket of USP7 .
    USP7 activator 1
  • HY-15252
    Reparixin L-lysine salt
    50+ Cited Publications

    Repertaxin L-lysine salt

    CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
    Reparixin L-lysine salt
  • HY-103269
    BAI1
    5+ Cited Publications

    Bcl-2 Family Apoptosis Cancer
    BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death .
    BAI1
  • HY-110031
    BAI1 hydrochloride
    5+ Cited Publications

    Apoptosis Bcl-2 Family Cancer
    BAI1 hydrochloride is a selective apoptosis factor BAX allosteric inhibitors. BAI1 hydrochloride binds BAX and allosterically inhibits its activation. BAI1 hydrochloride has the potential to be used in the study of BAX dependent cell death-mediated diseases .
    BAI1 hydrochloride
  • HY-169013

    Phosphatase Others
    DDO-3733 is a TRP-independent Protein Phosphatase 5 (PP5) allosteric activator that promotes dephosphorylation of downstream substrates .
    DDO-3733
  • HY-157508
    VCP Activator 1
    1 Publications Verification

    p97 Others
    VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail .
    VCP Activator 1
  • HY-15251
    Reparixin
    50+ Cited Publications

    Repertaxin; DF 1681Y

    CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    Reparixin
  • HY-103683
    PF-06409577
    1 Publications Verification

    AMPK Metabolic Disease
    PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
    PF-06409577
  • HY-17537
    APY29
    5+ Cited Publications

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
    APY29
  • HY-114589

    mGluR Others
    VU0240382 is a metabotropic glutamate receptor subtype 5 modulator whose activity differs depending on whether it has allosteric agonist activity. VU0240382 with allosteric agonist activity can activate mGlu(5) receptors in cell lines, but has no agonist activity in natural systems and has similar efficacy to mGlu(5) modulators without allosteric agonist activity in animal models.
    VU0240382
  • HY-N0197
    Baicalin
    25+ Cited Publications

    Baicalein 7-O-β-D-glucuronide

    NF-κB Autophagy HIV Inflammation/Immunology Cancer
    Baicalin, as a flavonoid glycoside, is an allosteric carnitine palmityl transferase 1 (CPT1) activator. Baicalin reduces the expression of NF-κB .
    Baicalin
  • HY-161928

    Glutathione Peroxidase Ferroptosis Cancer
    GPX4 activator 1 (Compound A9) is a allosteric activator of GPX4 (Kd = 5.86 μM, EC50 = 19.19 μM). GPX4 activator 1 can selectively act on ferroptosis and prevent the accumulation of intracellular lipid peroxides caused by ferroptosis inducers .
    GPX4 activator 1
  • HY-123661

    Endogenous Metabolite Neurological Disease
    MIPS1455 is a light-activated M1 muscarinic acetylcholine receptor ligand with irreversible binding activity to the allosteric site of the receptor. MIPS1455 is a drug target under investigation for the suppression of cognitive deficits and may become a valuable molecular tool for further investigation of allosteric interactions of the receptor .
    MIPS1455
  • HY-109128
    Danicamtiv
    1 Publications Verification

    MYK-491

    Myosin Cancer
    Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .
    Danicamtiv
  • HY-19330
    DASA-58
    10+ Cited Publications

    Pyruvate Kinase Metabolic Disease Cancer
    DASA-58 is a potential pyruvate kinase isozyme (PKM2) allosteric activator. DASA-58 can be used for the research of metabolism and kinds of cancer .
    DASA-58
  • HY-N2370
    24-Hydroxycholesterol
    2 Publications Verification

    iGluR LXR Neurological Disease
    24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
    24-Hydroxycholesterol
  • HY-17592
    Bithionol
    2 Publications Verification

    Parasite Bacterial Infection Cancer
    Bithionol is an antibacterial, anthelmintic, and algaecide agent. Bithionol is also a potent inhibitor of soluble adenylyl cyclase through binding to the allosteric activator site (IC50: 4 μM) .
    Bithionol
  • HY-18286

    TSH Receptor Endocrinology
    NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease .
    NCGC00229600
  • HY-114164D

    Thrombin Cardiovascular Disease
    Rat Thrombin is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins .
    Rat Thrombin
  • HY-114164F

    Thrombin Cardiovascular Disease
    Canine Thrombin is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins .
    Canine Thrombin
  • HY-114164E

    Thrombin Cardiovascular Disease
    Rabbit Thrombin is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins .
    Rabbit Thrombin
  • HY-10595
    RO-28-1675
    2 Publications Verification

    Glucokinase Metabolic Disease
    RO-28-1675 is a potent allosteric glucokinase (GK) activator with an EC50 of 54 nM. RO-28-1675 can be used for the research of type 2 diabetes .
    RO-28-1675
  • HY-101455
    CDN1163
    10+ Cited Publications

    Calcium Channel Metabolic Disease
    CDN1163 is an allosteric sarco/endoplasmic reticulum Ca 2+-ATPase (SERCA) activator that improves Ca 2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders .
    CDN1163
  • HY-114164G

    Thrombin Cardiovascular Disease
    Murine Thrombin is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins .
    Murine Thrombin
  • HY-114164
    Thrombin (MW 37kDa)
    5+ Cited Publications

    Thrombin Neurological Disease
    Thrombin (MW 37kDa) is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins.
    Thrombin  (MW 37kDa)
  • HY-115627
    PKUMDL-LC-101-D04
    3 Publications Verification

    GPX4-Activator-1d4

    Glutathione Peroxidase Inflammation/Immunology
    PKUMDL-LC-101-D04 (GPX4-Activator-1d4) is a glutathione peroxidase 4 (GPX4) allosteric activator (pEC50=4.7). PKUMDL-LC-101-D04 can inhibit ferroptosis and inflammation .
    PKUMDL-LC-101-D04
  • HY-115575

    Neuropeptide Y Receptor Metabolic Disease
    tBPC is a selective positive allosteric modulator for human Y4 receptor (Y4R), which enhances the activation of Y4R in G protein signaling and arrestin3 recruitment .
    tBPC
  • HY-106199
    Adenosine A1 receptor activator T62
    1 Publications Verification

    Adenosine Receptor Neurological Disease Inflammation/Immunology
    Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain .
    Adenosine A1 receptor activator T62
  • HY-10167

    R-568; NPS R-568 free base

    CaSR Others
    Tecalcet (R 568), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet (R 568) increases the sensitivity to activation by extracellular Ca 2+ .
    Tecalcet
  • HY-10167A
    Tecalcet Hydrochloride
    5+ Cited Publications

    R-568 hydrochloride; NPS R-568

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+ .
    Tecalcet Hydrochloride
  • HY-156757

    Sirtuin Cancer
    MDL-811, an allosteric SIRT6 activator, significantly activates SIRT6 histone H3 deacetylation (H3K9Ac, H3K18Ac, and H3K56Ac). MDL-811 could be used in the study of colorectal cancer .
    MDL-811
  • HY-129527

    iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity .
    GNE-9278
  • HY-150210

    Estrogen Receptor/ERR Endocrinology
    FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR .
    FSHR agonist 1
  • HY-161753

    CFTR Inflammation/Immunology
    CFTR potentiator 1 (I1421) is a potent CFTR potentiator with an EC50 value of 64 nM. CFTR potentiator 1 allosterically activates a wide range of CF-causing mutants, such as ΔF508 and G551D CFTR .
    CFTR potentiator 1
  • HY-124867

    TSH Receptor Endocrinology
    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro .
    D3-βArr
  • HY-158038

    Aurora Kinase Mitosis Cancer
    AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA .
    AurkA allosteric-IN-1
  • HY-N0197R

    NF-κB Autophagy HIV Inflammation/Immunology Cancer
    Baicalin (Standard) is the analytical standard of Baicalin. This product is intended for research and analytical applications. Baicalin, as a flavonoid glycoside, is an allosteric carnitine palmityl transferase 1 (CPT1) activator. Baicalin reduces the expression of NF-κB .
    Baicalin (Standard)
  • HY-15251A

    (Rac)-Repertaxin; (Rac)-DF 1681Y

    CXCR Inflammation/Immunology Endocrinology Cancer
    (Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    (Rac)-Reparixin
  • HY-14569
    CDPPB
    1 Publications Verification

    mGluR Akt ERK Caspase Mitochondrial Metabolism Neurological Disease
    CDPPB is a selective, orally active mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease .
    CDPPB