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Results for "

covalent antagonist

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-120188
    CC618

    		PPAR Others
    CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors .
    CC618
  • HY-112596A
    H3B-6545 hydrochloride
    3 Publications Verification

    		 Estrogen Receptor/ERR Cancer
    H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .
    H3B-6545 hydrochloride
  • HY-112596
    H3B-6545
    3 Publications Verification

    		 Estrogen Receptor/ERR Cancer
    H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .
    H3B-6545
  • HY-112693
    H-151
    Maximum Cited Publications
    108 Publications Verification

    		 STING Inflammation/Immunology
    H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease .
    H-151
  • HY-170382
    ER covalent antagonist-1

    		Estrogen Receptor/ERR Apoptosis Cancer
    ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
    ER covalent antagonist-1
  • HY-144733
    ERα antagonist 1

    		Estrogen Receptor/ERR Apoptosis Cancer
    ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
    ERα antagonist 1
  • HY-145823
    EGFR-IN-42

    		EGFR Cancer
    EGFR-IN-42 (Compound 17b) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity .
    EGFR-IN-42
  • HY-145824
    EGFR-IN-43

    		EGFR Cancer
    EGFR-IN-43 (Compound 17c) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-43 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-43 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-43 has superior anti-cancer activity .
    EGFR-IN-43
  • HY-135698
    Methocinnamox

    M-CAM

    		 Opioid Receptor Neurological Disease
    Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction .
    Methocinnamox
  • HY-175761
    Riboswit-modulator-1

    		Bacterial Infection
    Riboswit-modulator-1 (Compound A1), a covalent RNA ligand, is a bacterial Flavin mononucleotide (FMN) riboswitch modulator. Riboswit-modulator-1 modifies unpaired guanine residues (G11 and G62) proximal to the FMN-binding site through a proximity-driven mechanism, and interferes with its conformational transitions. Riboswit-modulator-1 acts as a negative antagonist by eliciting the opposite effect of the natural effector molecule .
    Riboswit-modulator-1
  • HY-112611
    H3B-5942

    		Estrogen Receptor/ERR Cancer
    H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations .
    H3B-5942
  • HY-N2909
    Aurantiamide

    		NF-κB RIP kinase Mixed Lineage Kinase Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Aurantiamide is a non-covalent, orally active, blood-brain-permeable GRPR selective antagonist with anti-inflammatory and neuroprotective effects. Aurantiamide reduces inflammation and oxidative stress in renal tissue by inhibiting GRPR-mediated renal necrosis pathways (such as RIPK3/MLKL signaling) and NF-κB inflammatory pathways, exerting anti-acute kidney injury and endothelial function activities. Aurantiamide also inhibits the M1 polarization of microglia and inhibits NLRP3 activation, thereby improving AD mouse models. Aurantiamide has in vivo inhibitory efficacy in acute kidney injury models such as ischemia/reperfusion, sepsis, and hypertension models .
    Aurantiamide

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