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Results for "

Small molecule antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Receptor (1) Androgen Receptor (1) Apoptosis (2) Aryl Hydrocarbon Receptor (1) CCR (1) CXCR (2) Endogenous Metabolite (1) Factor Xa (1) Integrin (2) Neuropeptide Y Receptor (1) Orexin Receptor (OX Receptor) (1) Protease Activated Receptor (PAR) (1) RAR/RXR (1) Smo (1) TNF Receptor (1) Toll-like Receptor (TLR) (1) TRP Channel (1) TSH Receptor (1) WDR5 (1)
By Research Areas:	Cancer (9) Cardiovascular Disease (2) Endocrinology (3) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (3)

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Fluorescent Dye

Biochemical Assay Reagents

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Targets Recommended: Small Interfering RNA (siRNA) ALCAM/CD166

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15412

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

HY-18668

Integrin Antagonists 27	Integrin	Cancer
Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent.

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.

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 .

HY-142214

TRPA1-IN-1	TRP Channel	Others
TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.

HY-158100

SYD5115	TSH Receptor	Endocrinology
SYD5115 is an orally available TSH-R antagonist .

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 pK_i of 6.4 for hPAR2 .

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 .

HY-131952

TLR7/8/9-IN-1 1 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).

HY-118922

IW927	TNF Receptor	Inflammation/Immunology
IW927 is a potent small molecule antagonist that blocks the binding of TNF-α to TNFRc1 with an IC₅₀ value of 50 nM and disrupts TNFα-induced IκB phosphorylation with an IC₅₀ value of 600 nM .

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 T_reg 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 .

HY-15001G

Stemregenin 1 (GMP) SR1 (GMP)	Aryl Hydrocarbon Receptor	Cancer
Stemregenin 1 (GMP) (SR1 (GMP)) is Stemregenin 1 Y-15001) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC₅₀ of 127 nM.

HY-125856

Milvexian BMS-986177; JNJ-70033093	Factor Xa	Cardiovascular Disease
Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the K_i 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 .

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 .

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.

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 .

HY-149434

PROTAC AR-NTD degrader 1	Androgen Receptor 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 .

HY-124637

ALE-0540	Others	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 treatment of pain .

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 .

HY-19767A

GSK 3008348 hydrochloride 2 Publications Verification	Integrin	Cardiovascular Disease
GSK 3008348 hydrochloride is a small molecule integrin αvβ6 antagonist, extracted from patent WO/2014154725A1, example 1. The affinity (pIC50) for the human - a 6 protein in the Fluorescence Polarisation Assay for GSK 3008348 (hydrochloride) is 8.1, whereas its affinity in the cell Adhesion Assays was for: ανβ6 (pIC50 = 8.4); ανβ3 (pIC50 = 6); ανβ5 (pIC50 = 6.9); ανβ8 (pIC50 = 7.7).

HY-30004

1-Aminocyclopropane-1-carboxylic acid	Endogenous Metabolite	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 protects neuron cells from death in in vivo ischemia models by moderately activating NMDA receptors. 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 shows promise for research in the field of neurotoxicity. .

Cat. No.	Product Name	Type

HY-U00449G

AGN 193109 (GMP)	Fluorescent Dye
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 (GMP)

Fluorescent Dye

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.

Cat. No.	Product Name	Type

HY-U00449G

AGN 193109 (GMP)	Biochemical Assay Reagents
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 (GMP)

Biochemical Assay Reagents

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-30004

1-Aminocyclopropane-1-carboxylic acid	Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
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 protects neuron cells from death in in vivo ischemia models by moderately activating NMDA receptors. 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 shows promise for research in the field of neurotoxicity. .

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Small molecule antagonist

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

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