Search Result

Results for "

allosteric effects

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Receptor (2) Akt (1) Apoptosis (1) Bacterial (1) Cholinesterase (ChE) (1) Discoidin Domain Receptor (1) DNA/RNA Synthesis (1) Dopamine Receptor (7) Dopamine Transporter (1) E1/E2/E3 Enzyme (1) GABA Receptor (1) Glutaminase (2) Histamine Receptor (5) HIV (1) iGluR (1) Isotope-Labeled Compounds (2) mAChR (7) mGluR (4) NF-κB (1) Phosphatase (1) PI3K (1) Potassium Channel (1) Prostaglandin Receptor (1) Reactive Oxygen Species (1) RGS Protein (1) Sodium Channel (1) Trk Receptor (1)
By Research Areas:	Cancer (15) Cardiovascular Disease (2) Infection (1) Inflammation/Immunology (4) Metabolic Disease (1) Neurological Disease (18)

By Targets:

Adenosine Receptor (2)

Akt (1)

Apoptosis (1)

Bacterial (1)

Cholinesterase (ChE) (1)

Discoidin Domain Receptor (1)

DNA/RNA Synthesis (1)

Dopamine Receptor (7)

Dopamine Transporter (1)

E1/E2/E3 Enzyme (1)

GABA Receptor (1)

Glutaminase (2)

Histamine Receptor (5)

HIV (1)

iGluR (1)

Isotope-Labeled Compounds (2)

mAChR (7)

mGluR (4)

NF-κB (1)

Phosphatase (1)

PI3K (1)

Potassium Channel (1)

Prostaglandin Receptor (1)

Reactive Oxygen Species (1)

RGS Protein (1)

Sodium Channel (1)

Trk Receptor (1)

By Research Areas:

Cancer (15)

Cardiovascular Disease (2)

Infection (1)

Inflammation/Immunology (4)

Metabolic Disease (1)

Neurological Disease (18)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-120837

PZ-II-029	GABA Receptor	Neurological Disease
PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .

HY-10915

LUF6096	Adenosine Receptor	Cardiovascular Disease
LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury .

HY-139644

MIPS521	Adenosine Receptor	Neurological Disease
MIPS521 is a positive allosteric modulator of adenosine A₁ receptor (A₁AR). MIPS521 also has a lower A₁R allosteric affinity (pK_B=4.95; K_B=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine .

HY-107111

GSK1034702	Cholinesterase (ChE)	Neurological Disease
GSK1034702 is a M1 mAChR allosteric agonist. GSK1034702 shows procognitive effects in rodents. GSK1034702 modulates hippocampal function to improve memory encoding in nicotine abstinence model of cognitive dysfunction .

HY-137067

IMT1B 5 Publications Verification LDC203974	DNA/RNA Synthesis	Cancer
IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects .

HY-145684

EP2 receptor antagonist-1	Prostaglandin Receptor	Inflammation/Immunology
EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects .

HY-151949

TrkA-IN-4	Trk Receptor	Neurological Disease
TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC₅₀=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects .

HY-163180

AKT-IN-22	Akt	Cancer
AKT-IN-22 (compound 0R4) is a potent AKT allosteric inhibitor with anticancer effects .

HY-128783

VU0090157	mAChR	Neurological Disease
VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .

HY-107663

MIF-1 Pro-Leu-Gly-NH2; Melanostatin	Dopamine Receptor	Neurological Disease
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .

HY-154848

UCL-TRO-1938 1 Publications Verification	PI3K	Cancer
UCL-TRO-1938 is a potent allosteric activator of PI3Kα with an EC₅₀ value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects .

HY-110180

VU0409106	mGluR	Neurological Disease
VU0409106 is a potent and selective mGlu₅ negative allosteric modulator (NAM) with an IC₅₀ of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .

HY-100979

W-84 dibromide HDMPPA	mAChR	Others
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ ³H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .

HY-107663A

MIF-1 TFA Pro-Leu-Gly-NH2 TFA; Melanostatin TFA	Dopamine Receptor	Neurological Disease
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .

HY-156331

VU6004909	mGluR	Neurological Disease
VU6004909 is a mGlu5 receptor positive allosteric modulator (pEC₅₀: 7.59). VU6004909 shows antipsychotic-like effects. VU6004909 can reverse MK801-induced cortical hyperactivity and cognitive deficits .

HY-B0520AS1

Benztropine-d3 mesylate	Dopamine Receptor Histamine Receptor mAChR	Cancer
Benztropine-d₃ (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].

HY-152207

LWG-301	Glutaminase Apoptosis	Cancer
LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC₅₀ value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model .

HY-B0520AS

Benztropine-13C,d3 mesylate	Isotope-Labeled Compounds Dopamine Receptor mAChR Histamine Receptor	Neurological Disease Cancer
Benztropine- ¹³C,d₃ (mesylate) is the ¹³C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].

HY-149602

Glutaminase C-IN-2	Glutaminase Reactive Oxygen Species	Cancer
Glutaminase C-IN-2 (compound 11) is glutaminase C (GAC) allosteric inhibitor with an IC₅₀ of 10.64 nM. Glutaminase C-IN-2 regulates the cellular metabolite, thereby increasing reactive oxygen species (ROS) by blocking glutamine metabolism. Glutaminase C-IN-2 has anticancer effects .

HY-B0520A

Benztropine mesylate 4 Publications Verification Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate	Dopamine Receptor mAChR Histamine Receptor	Neurological Disease Cancer
Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D₂ dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-B0520

Benztropine Benzatropine; Benzotropine	Dopamine Receptor mAChR Histamine Receptor	Cancer
Benztropine (Benzatropine; Benzotropine) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research . Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D₂ dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-N0240

Herbacetin 4 Publications Verification	Others	Cancer
Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .

HY-100939

4-Chlorophenylguanidine hydrochloride	Sodium Channel	Neurological Disease
4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo .

HY-114169S

WRG-28-d5	Isotope-Labeled Compounds	Cancer
WRG-28-d5 is the deuterium labeled WRG-28(HY-114169).WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC₅₀ of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic

HY-114169

WRG-28	Discoidin Domain Receptor	Inflammation/Immunology Cancer
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC₅₀ of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice .

HY-B0520AR

Benztropine mesylate (Standard) Benzatropine mesylate (Standard); Benzotropine mesylate (Standard); Benztropine methanesulfonate (Standard)	Dopamine Receptor mAChR Histamine Receptor	Neurological Disease Cancer
Benztropine (mesylate) (Standard) is the analytical standard of Benztropine (mesylate). This product is intended for research and analytical applications. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D₂ dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-49444

EN450	NF-κB E1/E2/E3 Enzyme	Cancer
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .

HY-120327

KY-226 1 Publications Verification	Phosphatase	Neurological Disease Metabolic Disease
KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC₅₀ of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury .

HY-161296

TH6342	Bacterial HIV	Infection
TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe .

HY-N0240R

Herbacetin (Standard)	Others	Cancer
Herbacetin (Standard) is the analytical standard of Herbacetin. This product is intended for research and analytical applications. Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .

HY-103565

AMN082	mGluR	Neurological Disease
AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀ values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .

HY-117902

SRI-31142	Dopamine Transporter	Neurological Disease
SRI-31142 is a putative, brain-penetrant allosteric inhibitor of the dopamine transporter (DAT). In behavioral studies using intracranial self-stimulation (ICSS), SRI-31142 did not produce the abuse-related effects seen with cocaine and GBR-12935, but instead reduced ICSS responses and dopamine levels in the nucleus accumbens (NAc) at effective doses. SRI-31142 also blocked cocaine-induced increases in ICSS and NAc dopamine .

HY-13509

CCG-50014 2 Publications Verification	RGS Protein	Inflammation/Immunology
CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC₅₀ =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site . CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test .

HY-120355A

AP14145 hydrochloride	Potassium Channel	Cardiovascular Disease
AP14145 hydrochloride is a potent K_Ca2 (SK) channel negative allosteric modulator with an IC₅₀ of 1.1 μM for K_Ca2.2 (SK2) and K_Ca2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF) .

HY-103565A

AMN082 free base	mGluR	Neurological Disease
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀ values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .

HY-156025

HCAR2 agonist 1	Others	Inflammation/Immunology
HCAR2 agonist 1 (Compound 9n) is a G_i protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the G_i protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .

HY-117734

PYD-106	iGluR	Neurological Disease
PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC₅₀. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library	187 compounds
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands. MCE designs a unique collection of 187 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Allosteric Modulators (AMs) Compound Library

187 compounds

An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.

MCE designs a unique collection of 187 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Cat. No.	Product Name	Target	Research Area

HY-107663A

MIF-1 TFA Pro-Leu-Gly-NH2 TFA; Melanostatin TFA	Dopamine Receptor	Neurological Disease
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .

HY-107663

MIF-1 Pro-Leu-Gly-NH2; Melanostatin	Dopamine Receptor	Neurological Disease
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0240

Herbacetin 4 Publications Verification	Flavonols Structural Classification Flavonoids Linum usitatissimum Linn. Classification of Application Fields Linaceae Source classification Phenols Polyphenols Plants Disease Research Fields Cancer	Others
Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .

HY-N0240R

Herbacetin (Standard)	Flavonols Structural Classification Flavonoids Linum usitatissimum Linn. Linaceae Source classification Phenols Polyphenols Plants	Others
Herbacetin (Standard) is the analytical standard of Herbacetin. This product is intended for research and analytical applications. Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .

Cat. No.	Product Name	Chemical Structure

HY-B0520AS1

Benztropine-d3 mesylate

Benztropine-d₃ (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].

HY-B0520AS

Benztropine-13C,d3 mesylate

Benztropine- ¹³C,d₃ (mesylate) is the ¹³C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].

HY-114169S

WRG-28-d5
WRG-28-d5 is the deuterium labeled WRG-28(HY-114169).WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC₅₀ of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic

Inquiry Online

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
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks