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Small molecule antagonist

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34

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3

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3

GMP Molecules

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-125856
    Milvexian
    2 Publications Verification

    BMS-986177; JNJ-70033093

    		 Factor Xa Cardiovascular Disease
    Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the Ki of 0.11, 0.38, 0.64, 490, 350 nM for human, rabbit, dog, rat, mouse, respectively. Milvexian shows anti-thrombosis activity in vitro and in vivo, and can be used for thrombus study .
    Milvexian
  • HY-30004
    1-Aminocyclopropane-1-carboxylic acid

    		Environmental Pollutants Endogenous Metabolite Cardiovascular Disease Metabolic Disease
    1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
    1-Aminocyclopropane-1-carboxylic acid
  • HY-123617
    AZ8838

    		Protease Activated Receptor (PAR) Inflammation/Immunology
    AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2 .
    AZ8838
  • HY-15001G
    Stemregenin 1

    SR1

    		 Aryl Hydrocarbon Receptor Cancer
    Stemregenin 1 (SR1) (GMP) is a GMP-grade Stemregenin 1 (HY-15001). GMP-grade small molecules can be used as adjuvants in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with an IC50 of 127 nM. Stemregenin 1 (GMP) can competitively bind to AhR and inhibit its nuclear translocation, inhibiting osteoclastogenesis and promoting hematopoietic progenitor cell expansion by blocking the AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway. Stemregenin 1 (GMP) can be used for the study of osteoporosis, in vitro expansion of hematopoietic stem cells, and the study of the mechanism of bone metabolic diseases .
    Stemregenin 1
  • HY-19767
    GSK 3008348
    2 Publications Verification

    		 Integrin TGF-β Receptor Infection Inflammation/Immunology Cancer
    GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer .
    GSK 3008348
  • HY-15412
    HhAntag
    1 Publications Verification

    		 Smo Cancer
    HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway .
    HhAntag
  • HY-158100
    SYD5115

    		TSH Receptor Endocrinology
    SYD5115 is an orally available TSH-R antagonist .
    SYD5115
  • HY-111308
    RTI-118

    		Neuropeptide Y Receptor Neurological Disease
    RTI-118 is a novel small-molecule neuropeptide S receptor (NPSR) antagonist. RTI-118 can relieve agent addiction including selectively decrease self-administration .
    RTI-118
  • HY-159989
    UNC10142

    		Epigenetic Reader Domain Cancer
    UNC10142 (Compound 44) is a first-in-class small molecule antagonist of CHD1 that binds with an IC50 value of 1.7 μM. UNC10142 leads to a dose-dependent reduction in viability in PTEN-deficient prostate cancer cells .
    UNC10142
  • HY-19767A
    GSK 3008348 hydrochloride
    2 Publications Verification

    		 Integrin TGF-β Receptor Infection Inflammation/Immunology Cancer
    GSK 3008348 hydrochloride is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer .
    GSK 3008348 hydrochloride
  • HY-18668
    Integrin antagonist 27

    		Integrin Cancer
    Integrin antagonist 27 (Compound 27) is a small molecule integrin αvβ3 antagonist with an affinity of 18 nM. Integrin antagonist 27 can be combined with Paclitaxel (HY-B0015) to selectively target αvβ3-positive metastatic cancer cells. Integrin antagonist 27 is used as an anticancer agent .
    Integrin antagonist 27
  • HY-131952
    TLR7/8/9-IN-1
    2 Publications Verification

    		 Toll-like Receptor (TLR) Inflammation/Immunology
    TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC50 = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).
    TLR7/8/9-IN-1
  • HY-16994
    OICR-0547

    		WDR5 Cancer
    OICR-0547 is a negative control, closely related derivative of OICR-9429 (HY-16993). OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction. OICR-0547 is an inactive control compound that no longer binds to WDR5 .
    OICR-0547
  • HY-125475
    Rivipansel

    GMI-1070

    		 E-Selectin Cardiovascular Disease
    Rivipansel is a small-molecule glycomimetic pan-selectin antagonist with inhibitory activity against E-selectin and P-selectin. Rivipansel binds tightly to the lectin domain of E-selectin, and selectively blocks the recognition of CD62L by E-selectin without affecting the binding of PSGL-1 to E-selectin. Rivipansel functionally inhibits the adhesion of hematopoietic cells to endothelial cells, and is applicable to research related to sickle cell disease .
    Rivipansel
  • HY-172458
    Z-3578
    1 Publications Verification

    		 Mas-related G-protein-coupled Receptor (MRGPR) TNF Receptor Inflammation/Immunology
    Z-3578 is an orally active small-molecule antagonist of MrgX2 with potent antipseudoallergic activity, exhibiting a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppresses the release of β-hexosaminidase, significantly reduces the release of histamine and TNF-α, and decreases intracellular calcium flux. In a mouse pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation, and reduces serum histamine levels. Z-3578 can be used for the study of pseudoallergic reactions .
    Z-3578
  • HY-30004R
    1-Aminocyclopropane-1-carboxylic acid (Standard)

    		Reference Standards Endogenous Metabolite Cardiovascular Disease Metabolic Disease
    1-Aminocyclopropane-1-carboxylic acid (Standard) is the analytical standard of 1-Aminocyclopropane-1-carboxylic acid. This product is intended for research and analytical applications. 1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
    1-Aminocyclopropane-1-carboxylic acid (Standard)
  • HY-12301
    MK-3697

    		Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.
    MK-3697
  • HY-124072
    HL001

    		Cyclophilin LPL Receptor MDM-2/p53 Apoptosis Reactive Oxygen Species (ROS) Cancer
    HL001 is an orally active small molecule inhibitor of Cyclophilin A (CypA) and a receptor antagonist of Lysophosphatidic acid 1 (LPA1). HL001 induces cell cycle arrest and apoptosis of tumor cells by p53. HL001 stabilizes p53 by down-regulating G3BP1, inducing reactive oxygen species and DNA damage. HL001 disrupts the interaction between MDM2 and p53-72R in a CypA dependent manner. HL001 has antitumor activity. HL001 can also be used to study pulmonary fibrosis .
    HL001
  • HY-100224G
    SANT-1

    		Smo Hedgehog Cancer
    SANT-1 (GMP) is SANT-1 (HY-100224) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling .
    SANT-1
  • HY-125836
    CCR4 antagonist 2

    		CCR Endocrinology Cancer
    CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively .
    CCR4 antagonist 2
  • HY-129094
    ICT5040

    		CXCR Cancer
    ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells .
    ICT5040
  • HY-149434
    PROTAC AR-NTD degrader 1

    		Androgen Receptor PROTACs Apoptosis Cancer
    PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .
    PROTAC AR-NTD degrader 1
  • HY-124637
    ALE-0540

    		Trk Receptor Neurological Disease
    ALE-0540, a nonpeptidic small molecule, is a nerve growth factor receptor antagonist. ALE-0540 inhibits the binding of NGF to tyrosine kinase (Trk) A or both p75 and TrkA with IC50 values of 5.88 μM and 3.72 μM, respectively. ALE-0540 can be used to examine mechanisms leading to the development of agents for the study of pain .
    ALE-0540
  • HY-U00449G
    AGN 193109

    		RAR/RXR Cancer
    AGN 193109 (GMP) is AGN 193109 (HY-U00449) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AGN 193109 is a specific and highly effective retinoic acid receptor (RAR) antagonist . AGN 193109 (GMP) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AGN 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.
    AGN 193109
  • HY-117087
    K103

    		Phosphatase PANoptosis Cancer
    K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.
    K103
  • HY-149558
    CXCR4-IN-2

    		Apoptosis CXCR Cancer
    CXCR4-IN-2 (compound A1) is a bifunctional fluorinated small molecule that is a potent CXCR4 inhibitor with anticancer activity. CXCR4-IN-2 has cytotoxic (IC50: 60 μg/mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. CXCR4-IN-2 induces cell arrest in the G2/M phase and induces apoptosis .
    CXCR4-IN-2
  • HY-124668A
    CCR1 antagonist 13

    		CCR Others
    CCR1 antagonist 13 is a selective CCR1 small molecule antagonist .
    CCR1 antagonist 13
  • HY-142214
    TRPA1-IN-1

    		TRP Channel Others
    TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.
    TRPA1-IN-1
  • HY-122192
    ICAM-1988

    		Integrin Inflammation/Immunology
    ICAM-1988 is a small molecule lymphocyte function-associated antigen-1 (LFA-1) antagonist that disrupts the LFA-1/ICAM-1 interaction and has anti-inflammatory activity .
    ICAM-1988
  • HY-116473
    CFM-1

    		APC Cancer
    CFM-1 is a small molecule antagonist of CARP-1/APC-2 binding with an EC50 value of 4.1 μM. CFM-1 induces G2M cell cycle arrest and suppresses viabilities of human breast cancer cells .
    CFM-1
  • HY-159923
    BPRMU191

    		Opioid Receptor Neurological Disease
    BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .
    BPRMU191
  • HY-136702
    L-97-1

    		Adenosine Receptor Inflammation/Immunology
    L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
    L-97-1
  • HY-118273
    IPS-05002

    		Integrin Inflammation/Immunology Cancer
    IPS-05002 is an α5β1 antagonist. IPS-05002 can inhibit VEGF-stimulated human umbilical vein endothelial cell (HUVEC) proliferation, adhesion, and migration, and also suppresses tubular network formation. IPS-05002 can upregulate IKB-β, XRCC4, and downregulate Cdc6 in VEGF-induced HUVECs. IPS-05002 can be used for the study of tumor angiogenesis .
    IPS-05002
  • HY-179648
    CD28-IN-2

    		CD28 Inflammation/Immunology Cancer
    CD28-IN-2 is a selective CD28-B7 interaction (IC50: 22.4 μM) inhibitor that binds directly to CD28, with a Kd value of 24.1 μM. CD28-IN-2 inhibits CD28-driven immune activation and blocks T cell costimulation. CD28-IN-2 can be used for the study of antitumor immunity and immune-related disorders .
    CD28-IN-2

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