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weak bind

" in MedChemExpress (MCE) Product Catalog:

29

Inhibitors & Agonists

1

Peptides

7

Natural
Products

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148433
    SpdSyn binder-1

    		Parasite Infection Inflammation/Immunology
    SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria .
    SpdSyn binder-1
  • HY-N6648
    Cirsimaritin

    		GABA Receptor Neurological Disease
    Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin
  • HY-130845A
    AR antagonist 1 hydrochloride

    		Ligands for E3 Ligase Ligands for Target Protein for PROTAC Androgen Receptor Cancer
    AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020) .
    AR antagonist 1 hydrochloride
  • HY-111547
    M1001

    		HIF/HIF Prolyl-Hydroxylase Cancer
    M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research .
    M1001
  • HY-117475
    N-Acetylthyroxine

    		Thyroid Hormone Receptor Endocrinology
    N-Acetylthyroxine is a thyroid hormone analogue. N-Acetylthyroxine weakly binds to thyroxine-binding globulin (TBG) in isolated human serum .
    N-Acetylthyroxine
  • HY-137709
    2'2'-cGAMP

    		STING IFNAR Endogenous Metabolite Metabolic Disease
    2'2'-cGAMP, a synthetic CDN, binds STING in the immune response, inducing IFN-β. 2'2'-cGAMP binds weaker binding to STING than 2'3'-cGAMP (HY-100564) but stronger than other CDNs .
    2'2'-cGAMP
  • HY-130845
    AR antagonist 1

    		Ligands for E3 Ligase Ligands for Target Protein for PROTAC Cancer
    AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1
  • HY-106827
    Trimegestone

    RU 27987

    		 Progesterone Receptor Androgen Receptor Phosphatase Endocrinology
    Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
    Trimegestone
  • HY-168368
    exo-Tetrahydrocannabivarin

    		Cannabinoid Receptor Others
    exo-Tetrahydrocannabivarin (Compound 12) is a Δ 9,11-THC analogue. exo-Tetrahydrocannabivarin weakly binds to cannabinoid receptors (CB) (IC50: 1.4 μM). exo-Tetrahydrocannabivarin is active on both motor and analgesic aspects in mice .
    exo-Tetrahydrocannabivarin
  • HY-106827S1
    Trimegestone-13C,d3

    RU 27987-13C,d3

    		 Androgen Receptor Phosphatase Progesterone Receptor Isotope-Labeled Compounds Endocrinology
    Trimegestone- 13C,d3 is 13C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
    Trimegestone-13C,d3
  • HY-111139
    MS417
    4 Publications Verification

    GTPL7512

    		 Epigenetic Reader Domain HIV Infection Inflammation/Immunology
    MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
    MS417
  • HY-118922
    IW927

    		TNF Receptor Inflammation/Immunology
    IW927 is a photochemically enhanced TNF-α-TNFR1 interaction inhibitor that blocks the binding of TNF-α to TNFRc1 with an IC50 value of 50 nM. IW927 binds reversibly to the TNFRc1 with weak affinity (Kd = 40-100 μM), covalently modifies the receptor via a photochemical reaction, and does not bind the related cytokine receptors TNFRc2 or CD40. IW927 disrupts TNFα-induced IκB phosphorylation with an IC50 value of 600 nM. IW927 can be used to develop light-independent inhibitors .
    IW927
  • HY-112061
    8-OH-DPAT
    4 Publications Verification

    8-Hydroxy-DPAT

    		 5-HT Receptor Neurological Disease
    8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
    8-OH-DPAT
  • HY-P11354
    THR-123

    		TGF-β Receptor Apoptosis Interleukin Related Integrin Cadherin Inflammation/Immunology
    THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis .
    THR-123
  • HY-121149B
    (E/Z)-Droloxifene

    (E/Z)-3-Hydroxytamoxifen

    		 Estrogen Receptor/ERR Apoptosis Cancer
    (E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
    (E/Z)-Droloxifene
  • HY-134055
    Arachidonoyl-N,N-dimethyl amide

    Arachidonic acid-N,N-dimethyl amide

    		 Cannabinoid Receptor Metabolic Disease
    Anandamide (AEA) is an endogenous cannabinoid that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. The biological actions of AEA are terminated by cellular uptake and hydrolysis of the amide bond by the enzyme fatty acid amide hydrolase. Arachidonoyl-N,N-dimethyl amide is an analog of anandamide that exhibits weak or no binding to the human central cannabinoid (CB1) receptor (Ki >1 μM). It inhibits rat glial gap junction cell-cell communication 100% at a concentration of 50 μM.
    Arachidonoyl-N,N-dimethyl amide
  • HY-113038
    D-α-Hydroxyglutaric acid
    3 Publications Verification

    (R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid

    		 Reactive Oxygen Species (ROS) ATP Synthase mTOR Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling .
    D-α-Hydroxyglutaric acid
  • HY-135096
    Amitriptyline-d3 hydrochloride

    		Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor Neurological Disease
    Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
    Amitriptyline-d3 hydrochloride
  • HY-113421
    Linoleoyl ethanolamide

    Linoleic acid monoethanolamide

    		 Cannabinoid Receptor Neurological Disease
    Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
    Linoleoyl ethanolamide
  • HY-112061R
    8-OH-DPAT (Standard)

    		5-HT Receptor Neurological Disease
    8-OH-DPAT (Standard) is the analytical standard of 8-OH-DPAT. This product is intended for research and analytical applications. 8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
    8-OH-DPAT (Standard)
  • HY-100542
    D-α-Hydroxyglutaric acid disodium
    3 Publications Verification

    Disodium (R)-2-hydroxyglutarate

    		 Reactive Oxygen Species (ROS) ATP Synthase mTOR Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling .
    D-α-Hydroxyglutaric acid disodium
  • HY-113421S
    Linoleoyl ethanolamide-d4

    		Isotope-Labeled Compounds Cannabinoid Receptor Neurological Disease
    Linoleoyl ethanolamide-d4 is a deuterated labeled Linoleoyl ethanolamide . Linoleoyl ethanolamide (Linoleic acid monoethanolamide) is classified as a fatty acid ethanolamide. Linoleoyl ethanolamide only weakly binds G-protein-coupled cannabinoid receptors of type-1（CB1）and CB2 receptors, and inhibits the binding of [3H]CP-55,940 with Kis of 10 and 25 μM, respectively. Linoleoyl ethanolamide is 4-fold less potent than anandamide at causing catalepsy in mice and it does not prolong sleep time .
    Linoleoyl ethanolamide-d4
  • HY-113329
    Guanidinoethyl sulfonate
    4 Publications Verification

    Taurocyamine

    		 Endogenous Metabolite Metabolic Disease
    Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
    Guanidinoethyl sulfonate
  • HY-131968
    BMS-986202

    		JAK Cytochrome P450 Inflammation/Immunology
    BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium .
    BMS-986202
  • HY-113329R
    Guanidinoethyl sulfonate (Standard)

    		Endogenous Metabolite Metabolic Disease
    Guanidinoethyl sulfonate (Standard) is the analytical standard of Guanidinoethyl sulfonate. This product is intended for research and analytical applications. Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
    Guanidinoethyl sulfonate (Standard)
  • HY-100542R
    D-α-Hydroxyglutaric acid disodium (Standard)

    Disodium (R)-2-hydroxyglutarate (Standard)

    		 Reference Standards Reactive Oxygen Species (ROS) ATP Synthase mTOR Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    D-α-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of D-α-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling .
    D-α-Hydroxyglutaric acid disodium (Standard)
  • HY-111126
    K67
    1 Publications Verification

    		 p62 Keap1-Nrf2 Cancer
    K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2 .
    K67
  • HY-W654003
    D-α-Hydroxyglutaric acid-d5 disodium

    Disodium (R)-2-hydroxyglutarate-d5

    		 Reactive Oxygen Species (ROS) Neurological Disease Inflammation/Immunology Cancer
    D-α-Hydroxyglutaric acid-d5 disodium (Disodium (R)-2-hydroxyglutarate-d5) is the deuterium labeled D-α-Hydroxyglutaric acid disodium (HY-100542). D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling .
    D-α-Hydroxyglutaric acid-d5 disodium
  • HY-174301
    USP7-IN-18

    		Deubiquitinase DNA Methyltransferase MDM-2/p53 Cancer
    USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC50 : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins MDM2 and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions.
    USP7-IN-18

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