Search Result

Results for "

covalent antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Apoptosis (2) Bacterial (1) Dopamine Receptor (1) Drug Derivative (1) Drug Metabolite (1) EGFR (2) Estrogen Receptor/ERR (5) IFNAR (1) IKK (1) Interleukin Related (1) mAChR (1) Mixed Lineage Kinase (1) NF-κB (2) Opioid Receptor (1) P2Y Receptor (1) PPAR (3) RIP kinase (1) STING (2) TGF-beta/Smad (1) Toll-like Receptor (TLR) (1)
By Research Areas:	Cancer (10) Cardiovascular Disease (3) Infection (1) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (3)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Natural
Products

Click Chemistry

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-112693

H-151 Maximum Cited Publications 138 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 .

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 .

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 .

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 K_is 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 .

HY-112247

SR 16832	PPAR TGF-beta/Smad	Metabolic Disease Inflammation/Immunology
SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis .

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 .

HY-123669

R-138727	P2Y Receptor Drug Metabolite	Cardiovascular Disease
R-138727, the major active metabolite of Prasugrel (HY-15284), is a highly potent and selective irreversible antagonist of the P2Y12 receptor, with an IC₅₀ of 2.5 μM. R-138727 covalently binds to the P2Y12 receptor on the platelet surface, blocking adenosine diphosphate-mediated platelet activation and aggregation. R-138727 can be used to study stroke, cerebral infarction and neurological deficits.

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 .

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 .

HY-120188

CC618	PPAR	Others
CC618 is a selective PPARβ/δ antagonist. CC618 covalently modifies conserved Cys249 in the PPARβ/δ ligand-binding pocket via nucleophilic aromatic substitution, converting its thiol moiety to a 5-trifluoromethyl-2-pyridylthioether .

HY-135698

Methocinnamox M-CAM	Opioid Receptor	Neurological Disease
Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a K_i 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) (K_i = 4.9 nM) and delta-opioid receptor (DOR) (K_i = 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 .

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 .

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 .

HY-180507

TLR2/9 antagonist 1	Toll-like Receptor (TLR)	Neurological Disease Inflammation/Immunology Cancer
TLR2/9 antagonist 1 (Compound 24) is a reversible covalent TLR2 (IC₅₀ = 0.5 μM (TLR2/TLR6); IC₅₀ = 0.6 μM (TLR2/TLR1)) and TLR9 (IC₅₀ = 0.32 μM) antagonist. TLR2/9 antagonist 1 has no significant effect on other TLR subtypes. TLR2/9 antagonist 1 can be used for studying central nervous system diseases and malignant tumors caused by inflammation .

HY-181427

UT-143	Androgen Receptor	Cancer
UT-143 is an orally active, selective irreversible covalent antagonist of androgen receptor (AR). UT-143 inhibits the proliferation of AR-positive prostate cancer cells, reduces the weight of androgen target tissues in rats, and suppresses the growth of AR-positive xenograft tumors. UT-143 can be used for the research of prostate cancer .

HY-122222

MRL20	PPAR	Others
MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC₅₀ being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC₅₀ values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ .

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 .

HY-180120

UM-203	STING IKK NF-κB IFNAR Interleukin Related	Inflammation/Immunology
UM-203 is a reversible covalent STING antagonist. UM-203 is effective against both mouse and human STING, and in particular, it inhibits the most common human STING R232 variant. UM-203 can inhibit STING oligomerization and reduce phosphorylation of downstream TBK1 and IRF3, thereby blocking the IRF3 and NF-κB-mediated signaling pathways and inhibiting IFNβ and IL-6 secretion. UM-203 can be used for the research of inflammation and immunology, such as systemic lupus erythematosus .

HY-186083

Propylbenzilylcholine mustard	mAChR	Cardiovascular Disease
Propylbenzilylcholine mustard (PrBCM) is an irreversible, covalently binding selective antagonist targeting rat cardiac muscarinic receptors, with a preference for muscarinic receptor subtypes that show low affinity for agonists. Propylbenzilylcholine mustard inactivates such receptors in a dose- and time-dependent manner in vitro, and its receptor selectivity remains stable across different ionic strengths and in GTP-containing buffer systems. Propylbenzilylcholine mustard can be applied to basic pharmacological studies on the structure and function of muscarinic receptors, especially focusing on the heterogeneity of cardiac muscarinic receptors and related cardiovascular pharmacological research .

HY-180814

SKF-83566-PEG1-pomalidomide	Drug Derivative Dopamine Receptor	Cancer
SKF-83566-PEG1-pomalidomide is an anti-tumor agent and is formed by the covalent connection of SKF-83566 (HY-103430A) (dopamine D1 receptor antagonist) and Pomalidomide (HY-10984) (immunomodulatory agent). SKF-83566-PEG1-pomalidomide can inhibit cancer cells invasion, migration and colony formation. SKF-83566-PEG1-pomalidomide can inhibit tumor growth and angiogenesis in MDA-MB-231 cell chicken embryo chorioallantoic membrane (CAM) xenograft model. SKF-83566-PEG1-pomalidomide can be used for research of breast cancer .

Cat. No.	Nombre del producto	Category	Target	Chemical Structure

HY-N2909

Aurantiamide	Alkaloids Classification of Application Fields Other Alkaloids Umbelliferae Plants Inflammation/Immunology Disease Research Fields Carphephorus corymbosus (Nutt.) Torr. & A.Gray Source Classification	NF-κB RIP kinase Mixed Lineage Kinase
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 .

Cat. No.	Nombre del producto		Classification

HY-180120

UM-203		Alkynes
UM-203 is a reversible covalent STING antagonist. UM-203 is effective against both mouse and human STING, and in particular, it inhibits the most common human STING R232 variant. UM-203 can inhibit STING oligomerization and reduce phosphorylation of downstream TBK1 and IRF3, thereby blocking the IRF3 and NF-κB-mediated signaling pathways and inhibiting IFNβ and IL-6 secretion. UM-203 can be used for the research of inflammation and immunology, such as systemic lupus erythematosus .

Consulta en línea

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Saludo			Country or Region *
Nombre del solicitante *			Nombre de la Organizaciòn *
Department *
Direcciòn del E-mail *			Nombre del producto *
Cat. No.			Requested quantity *
Número de teléfono *
Observaciones

Consulta en línea

Inquiry Information

Nombre del producto:
Cat. No.:
Cantidad:
MCE Japan Authorized Agent:

Name
E-mail *

	Sorry, but the email address you supplied was invalid.

covalent antagonist

Inhibitors & Agonists

NaturalProducts

Click Chemistry

Natural
Products