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Results for "

balanced inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Adenosine Receptor (1) Akt (1) Amyloid-β (1) Angiotensin Receptor (1) Apoptosis (1) Arrestin (1) Beta-secretase (1) Calcium Channel (1) CDK (1) Cholinesterase (ChE) (2) Dopamine Receptor (3) Epigenetic Reader Domain (1) ERK (1) G protein-coupled Bile Acid Receptor 1 (1) GCGR (1) GLP Receptor (1) GSK-3 (1) HDAC (1) Isotope-Labeled Compounds (1) Neuropeptide Y Receptor (1) P-glycoprotein (1) Photosensitizer (1) PI3K (1) Pim (1) PKA (1) Potassium Channel (1) Sodium Channel (1) Somatostatin Receptor (1) Tau Protein (1) Transmembrane Glycoprotein (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (2) Metabolic Disease (2) Neurological Disease (7)

By Targets:

5-HT Receptor (3)

Adenosine Receptor (1)

Akt (1)

Amyloid-β (1)

Angiotensin Receptor (1)

Apoptosis (1)

Arrestin (1)

Beta-secretase (1)

Calcium Channel (1)

CDK (1)

Cholinesterase (ChE) (2)

Dopamine Receptor (3)

Epigenetic Reader Domain (1)

ERK (1)

G protein-coupled Bile Acid Receptor 1 (1)

GCGR (1)

GLP Receptor (1)

GSK-3 (1)

HDAC (1)

Isotope-Labeled Compounds (1)

Neuropeptide Y Receptor (1)

P-glycoprotein (1)

Photosensitizer (1)

PI3K (1)

Pim (1)

PKA (1)

Potassium Channel (1)

Sodium Channel (1)

Somatostatin Receptor (1)

Tau Protein (1)

Transmembrane Glycoprotein (1)

By Research Areas:

Cancer (5)

Cardiovascular Disease (2)

Metabolic Disease (2)

Neurological Disease (7)

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-50862

Akt1/Akt2-IN-1 2 Publications Verification	Akt	Cancer
Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC₅₀=3.5 nM) and Akt2 (IC₅₀=42 nM), with potent and balanced activity .

HY-14834A

Budiodarone tartrate ATI-2042 tartrate	Potassium Channel Sodium Channel Calcium Channel	Cardiovascular Disease
Budiodarone (ATI-2042) tartrate is a chemical analogue of Amiodarone (HY-14187) with balanced, multiple cardiac ion channel (potassium, sodium and calcium channels) inhibiting activity. Budiodarone tartrate is an antiarrhythmic agent .

HY-142696

CDK6/PIM1-IN-1	CDK Pim Apoptosis	Cancer
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC₅₀ values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC₅₀=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity .

HY-146260

NVP-CLR457	PI3K	Cancer
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .

HY-176287

ARN25657	Dopamine Receptor GSK-3 PKA P-glycoprotein	Neurological Disease
ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC₅₀ = 15.2 nM, K_i=1.5 nM) and potent GSK-3β inhibitor activity (IC₅₀ = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .

HY-106605

Flumezapine LY 120363	Dopamine Receptor 5-HT Receptor	Neurological Disease
Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .

HY-143324

A2AAR/HDAC-IN-1	HDAC Adenosine Receptor	Cancer
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A_2AAR/HDAC dual inhibitor, with a K_i of 163.5 nM for A_2AAR and an IC₅₀ of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity .

HY-161341

β-Glucuronidase responsive conjugate 1	Photosensitizer	Cancer
β-Glucuronidase responsive conjugate 1 (compound 3) is a well-balanced photosensitizer which has photodynamic activity. β-Glucuronidase responsive conjugate 1 inhibits T-24 cell viability and growth with an IC₅₀ of 0.2 μM. β-Glucuronidase responsive conjugate 1 can used to study bladder cancers .

HY-114284

L-163958	Angiotensin Receptor	Cardiovascular Disease
L-163958 is an efficient, orally active, balanced angiotensin II receptor (AII receptor) antagonist. L-163958 has balanced high affinity for AT1 and AT2, with its IC₅₀ values being 0.16, 0.12, 0.50, and 0.64 nM in rabbit aorta (AT1), rat midbrain (AT2), human adrenal gland (AT1), and human adrenal gland (AT2), respectively. L-163958 has a strong inhibitory effect on the pressor activity in rats. L-163958 can be used for the study of hypertension and related cardiovascular diseases .

HY-106605S

Flumezapine-d8 hydrochloride LY 120363-d8 hydrochloride	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
Flumezapine-d₈ (LY 120363-d₈) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.

HY-175658

AChE/BChE-IN-29	Cholinesterase (ChE) Amyloid-β Tau Protein	Neurological Disease
AChE/BChE-IN-29 is an AChE/BChE inhibitor. AChE/BChE-IN-29 exhibits balanced dual cholinesterase inhibitory activity with IC₅₀ values of 2.1 μM for Electrophorus electricus AChE (eeAChE) and 6.3 μM for equine serum butyrylcholinesterase (eqBChE). AChE/BChE-IN-29 effectively inhibits amyloid-β (Aβ₄₂) aggregation and tau protein aggregation in E. coli cell models. AChE/BChE-IN-29 can be used for the study of Alzheimer’s disease (AD) .

HY-157527

hAChE-IN-7	Cholinesterase (ChE) Beta-secretase	Neurological Disease
hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC₅₀=69.8 nM) and hBuChE (IC₅₀=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC₅₀=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .

HY-162585

5-HT1AR agonist 1	5-HT Receptor	Neurological Disease
5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC₅₀ value of 34 nM, SERT reuptake ihibitor (IC₅₀ =12 nM), NET reuptake inhibitor (IC₅₀ =78 nM) and DAT reuptake inhibitor (IC₅₀ =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .

HY-P11275

TC4	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
TC4 is a highly balanced single-molecule quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC₅₀ values of 0.95, 31, 81, and 1100 nM respectively. TC4 exhibits extremely strong signal bias on GLP-1R and has very low recruitment efficacy for β-inhibitor protein 2 (βArr2) and this strong cAMP preference is believed to maximize metabolic benefits (such as weight loss and hypoglycemia) while possibly minimizing side effects mediated by β-inhibitor protein recruitment (such as receptor desensitization). TC4 can be used for research on obesity and diabetes .

HY-179606

RWT9996	Transmembrane Glycoprotein Arrestin ERK Epigenetic Reader Domain	Neurological Disease
RWT9996 is a balanced GPR17 antagonist. RWT9996 has an inhibitory effect on G protein activation and β-arrestin-2 recruitment induced by MDL-29951. RWT9996 inhibits the phosphorylation of ERK/CREB and the accumulation of inositol phosphate (b IP1) induced by MDL-29951. RWT9996 can be used for the study of neurological diseases .

HY-182905

SSTR5/TGR5-modulator-1	Somatostatin Receptor G protein-coupled Bile Acid Receptor 1	Metabolic Disease
SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus .

Cat. No.	Product Name

HY-L110

Cyclic Peptide Library	97 compounds
Cyclic peptides are polypeptide chains taking cyclic ring structure, which exhibit diverse biological activities, such as antibacterial activity, immunosuppressive activity and anti-tumor activity. Cyclic peptides, with the features of good binding affinity, target selectivity and low toxicity, show great success as therapeutics. Multiple cyclic peptides are currently in clinical use, for examples, gramicidin and tyrocidine with bactericidal activity, cyclosporin A with immunosuppressive activity, and vancomycin with antibacterial activity. Furthermore, cyclic peptides usually have the sufficient size and a balanced conformational flexibility/rigidity for binding to flat protein-protein interaction (PPI) interfaces, which have potential to develop PPI drugs. MCE offers a unique collection of 97 cyclic peptides, all of which have good bioactivities. MCE Cyclic Peptide Library is a powerful tool for drug discovery and PPI inhibitor screening.

Cyclic Peptide Library

97 compounds

Cyclic peptides are polypeptide chains taking cyclic ring structure, which exhibit diverse biological activities, such as antibacterial activity, immunosuppressive activity and anti-tumor activity. Cyclic peptides, with the features of good binding affinity, target selectivity and low toxicity, show great success as therapeutics. Multiple cyclic peptides are currently in clinical use, for examples, gramicidin and tyrocidine with bactericidal activity, cyclosporin A with immunosuppressive activity, and vancomycin with antibacterial activity. Furthermore, cyclic peptides usually have the sufficient size and a balanced conformational flexibility/rigidity for binding to flat protein-protein interaction (PPI) interfaces, which have potential to develop PPI drugs.

MCE offers a unique collection of 97 cyclic peptides, all of which have good bioactivities. MCE Cyclic Peptide Library is a powerful tool for drug discovery and PPI inhibitor screening.

Cat. No.	Product Name	Target	Research Area

HY-P11275

TC4	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
TC4 is a highly balanced single-molecule quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC₅₀ values of 0.95, 31, 81, and 1100 nM respectively. TC4 exhibits extremely strong signal bias on GLP-1R and has very low recruitment efficacy for β-inhibitor protein 2 (βArr2) and this strong cAMP preference is believed to maximize metabolic benefits (such as weight loss and hypoglycemia) while possibly minimizing side effects mediated by β-inhibitor protein recruitment (such as receptor desensitization). TC4 can be used for research on obesity and diabetes .

Cat. No.	Product Name	Chemical Structure

HY-106605S

Flumezapine-d8 hydrochloride
Flumezapine-d₈ (LY 120363-d₈) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.

Flumezapine-d8 hydrochloride

Flumezapine-d₈ (LY 120363-d₈) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.

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