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Allosteric

" in MedChemExpress (MCE) Product Catalog:

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By Research Areas:	Cancer (272) Cardiovascular Disease (29) Endocrinology (24) Infection (57) Inflammation/Immunology (73) Metabolic Disease (70) Neurological Disease (361)
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862

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

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Isotope-Labeled Compounds

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*CB1R Allosteric* modulator 3**	Cannabinoid Receptor Arrestin	Neurological Disease
CB1R Allosteric modulator 3 is a *CB1R positive allosteric* modulator*. CB1R Allosteric* modulator 3 has potent inhibition of cAMP and β-Arrestin with EC₅₀ values of 0.018 μM and 1.241 μM, respectively .

*AurkA allosteric-IN-1*	Aurora Kinase	Cancer
AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC₅₀: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA .

*CB1R Allosteric* modulator 4**	Cannabinoid Receptor	Others
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .

*PCSK9 allosteric* binder-1**	PCSK9	Cardiovascular Disease
PCSK9 allosteric binder-1 (example 70) is a PCSK9 allosteric binder. PCSK9 allosteric binder-1 can be used in the study of cardiovascular diseases .

*ERK2 allosteric-IN-1*	ERK	Metabolic Disease Cancer
ERK2 allosteric-IN-1 (compound 1) is a selective and allosteric ERK2 inhibitor with the IC₅₀ of 11 μM .

*CB1R Allosteric* modulator 1**	Cannabinoid Receptor	Others
CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .

*CB1R Allosteric* modulator 2**	Cannabinoid Receptor	Others
CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .

*PDK1 allosteric* modulator 1**	Others	Others
PDK1 allosteric modulator 1 is a molecule targeting PDK1 with a binding affinity of 8 μM. PDK1 allosteric modulator 1 is able to bind to the PIF pocket of PDK1, potentially affecting the biological activity of this kinase .

*Integrase-LEDGF/p75 allosteric* inhibitor 1**	HIV Integrase	Infection
Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC₅₀ of 3.9 nM against HIV-1 recombinant molecular clone NL432 .

*Androgen receptor allosteric* antagonist 1**	Estrogen Receptor/ERR	Cancer
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the K_i of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .

Sadopine	Calcium Channel	Others
Sadopine is an allosteric modulator for dihydropyridine receptor ((-)Sadopine as positive allosteric modulator and (+)Sadopine as negative allosteric modulator). Sadopine interacts with dihydropyridine (DHP)-sensitive L-type calcium channels .

VUF8507	Adenosine Receptor	Others
VUF8507 is an allosteric modulator for adenosine A3 receptor with a K_i of 204 nM .

NVS-MALT1	MALT1	Cancer
NVS-MALT1 is a MALT1 allosteric inhibitor .

UKTT15	PARP	Cancer
UKTT15 (compound 6) is an allosteric inhibitor of PARP1 .

MHC00188	Phosphodiesterase (PDE)	Others Cancer
MHC00188 is an allosteric inhibitor for Autotaxin (ATX) with an IC₅₀ of 2.53 μM .

Aurkin A	Aurora Kinase	Cancer
Aurkin A is an allosteric inhibitor for the interaction between Aurora A Kinase (also known also Aurka) and TPX2, through targeting the TPX2 binding sites with K_d of 3.77 μM .

Brexanolone caprilcerbate	GABA Receptor	Neurological Disease
Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator .

AI-4-57	Others	Cancer
AI-4-57 is an allosteric inhibitor for CBFβ SMMHC-RUNX1 interaction with an IC₅₀ of 22 μM .

TMPPAA	5-HT Receptor	Neurological Disease
TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling .

CGP13501	GABA Receptor	Neurological Disease
CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol .

VU0366248	mGluR	Neurological Disease
VU0366248 is a mGlu5 negative allosteric modulator .

SHP836 1 Publications Verification	SHP2 Phosphatase	Cancer
SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2 .

VU6008677	Cytochrome P450 mAChR	Neurological Disease
VU6008677 is a positive allosteric modulator (PAM) for M4, with EC₅₀ of 120 nM for hM4. VU6008677 inhibits cytochrome P450, exhibits good pharmacokinetic characteristics in rats .

VU0404251	mGluR	Neurological Disease
VU0404251 is a highly potent positive allosteric modulator of mGlu for the study of psychosis .

4BP-TQS	nAChR	Neurological Disease
4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site .

U-89843A hydrochloride	GABA Receptor	Neurological Disease
U-89843A is an allosteric modulator of GABAA receptor. U-89843A enhances GABA-induced Cl ^- currents .

BZG2	SARS-CoV Virus Protease	Infection
BZG2 is an allosteric inhibitor for the SARS-CoV-2 main protease (M ^pro), with an IC₅₀ of 77 µM .

MRS7935	Adenosine Receptor	Endocrinology
MRS7935 (compound 15) is an A1AR positive allosteric modulator (PAM) with an EC₅₀ of approximately 2 μM .

DA-023	EAAT	Neurological Disease
DA-023 (Compound 4) is a selective positive allosteric modulator (PAM) of EAAT2 with an EC₅₀ value of 1 nM .

Refametinib 10+ Cited Publications BAY 869766; RDEA119	MEK	Cancer
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC₅₀s of 19 nM and 47 nM, respectively.

Direclidine	mAChR	Neurological Disease
Direclidine is a muscarinic M4 receptor positive allosteric modulator .

VU 0360223	mGluR	Neurological Disease
VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC₅₀ of 61 nM .

GPCR modulator-1	GCGR	Metabolic Disease
GPCR modulator-1 is a negative allosteric modulator of GLP receptor. GPCR modulator-1 has the potential for type 2 diabetes research .

VU0486846	mAChR	Neurological Disease
VU0486846 is an orally active and selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) .

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 .

D5261	Trk Receptor	Cancer
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor .

IGF-1R inhibitor-3	IGF-1R	Cancer
IGF-1R inhibitor-3 (Compound C11) is an allosteric inhibitor for insulin-like growth factor receptor 1 kinase (IGF-1R), with an IC₅₀ of 0.2 μM .

Calindol hydrochloride	CaSR	Cardiovascular Disease
Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC₅₀ of 132 nM .

TNF-α-IN-6	TNF Receptor	Inflammation/Immunology
TNF-α-IN-6 (compound 12) is an orally effective allosteric inhibitor of TNFα (K_D = 6.8 nM). TNF-α-IN-6 has anti-inflammatory effects .

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 .

DCB	mGluR	Neurological Disease
DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB) .

LUF6000 1 Publications Verification	Adenosine Receptor	Cardiovascular Disease
LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect .

VU6007496	Others	Neurological Disease
VU6007496 is a highly selective and CNS penetrant M1 positive allosteric modulator (PAM). VU6007496 shows excellent pharmacokinetics (PK) .

mGluR2 modulator 4	mGluR	Neurological Disease
mGluR2 modulator 4 (compound 47) is a potent mGluR2 positive allosteric modulator with an EC₅₀ value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic .

PHCCC(4Me) THCCC	mGluR	Neurological Disease
PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC₅₀ of 1.5 μM) negative allosteric modulator and mGluR3 (EC₅₀ of 8.9 μM) positive allosteric modulator .

A-286982 2 Publications Verification	Integrin	Inflammation/Immunology
A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC₅₀s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library

183 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 183 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Cat. No.	Product Name	Type

HY-137782

Palmitoleoyl-CoA	Biochemical Assay Reagents
Palmitoleoyl-CoA can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA induces the cardiac mitochondrial membrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA regulates metabolism via allosteric control of AMPK β1-isoforms .

Cat. No.	Product Name	Target	Research Area

HY-126327A

UNC4976 TFA	Histone Methyltransferase	Cancer
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

HY-P1397A

RVD-Hpα TFA	Cannabinoid Receptor	Cardiovascular Disease
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca ²⁺ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (K_i=50 nM).

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-P4910

Baceridin	Proteasome Apoptosis	Cancer
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research .

HY-P5860

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric GABA_A receptor modulator that increases GABA_A receptor susceptibility to agonist .

HY-P2120

Pseudobactin A	Peptides	Others
Pseudobactin A is a non-fluorescent extracellular iron carrier produced by the plant growth-promoting bacterium Pseudomonas B10 .

HY-P1397

RVD-Hpα	Cannabinoid Receptor	Neurological Disease
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2 .

HY-P1402

[Glu27]-PKC (19-36)	Peptides	Others
[Glu27]-PKC (19-36) is an inactive control for protein kinase C (PKC) (19-36). PKC (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C, it may be responsible for maintaining the enzyme in the inactive form in the absence of allosteric activators such as phospholipids .

HY-126327

UNC4976	Histone Methyltransferase	Cancer
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .

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-P1259

PR-39	Proteasome Bacterial	Inflammation/Immunology
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P1259A

PR-39 TFA	Proteasome Bacterial	Inflammation/Immunology
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P10436

Braftide	Raf	Cancer
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF ^G469A with IC₅₀ of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC₅₀ is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .

HY-P1045

187-1, N-WASP inhibitor 1 Publications Verification	Arp2/3 Complex	Others
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC₅₀ of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein .

HY-P1045A

187-1, N-WASP inhibitor TFA	Arp2/3 Complex	Others
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC₅₀ of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein .

HY-P4160

PDC31 THG113.31; ILGHXDYK	Prostaglandin Receptor	Endocrinology
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca ²⁺-dependent large-conductance K ⁺-channel in human myometrial cells .

HY-P0172A

ATI-2341 TFA 2 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P0172

ATI-2341	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

Cat. No.	Product Name	Target	Research Area

HY-P99171

Gevokizumab	Interleukin Related	Inflammation/Immunology Cancer
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .

Cat. No.	Product Name	Chemical Structure

HY-70037AS

Cinacalcet-d3 hydrochloride
Cinacalcet-d₃ (hydrochloride) is the deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-14774S

(Rac)-Monepantel-d5
(Rac)-Monepantel-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-14774S1

(Rac)-Monepantel sulfone-d5
(Rac)-Monepantel sulfone-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification
Tetrahydrodeoxycorticosterone-d₃ is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].

HY-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].

HY-15831

L-838417-d9
L-838417-d₉ is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

HY-70037S

Cinacalcet-D3
Cinacalcet-d₃ is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-10933S

CX516-d10
CX516-d₁₀ is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI)[1].

HY-13619S

Efaproxiral-d6
Efaproxiral-d₆ is the deuterium labeled Efaproxiral. Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy[1][2].

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].

HY-16579AS2

Etifoxine-d5
Etifoxine-d₅ is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].

HY-10046S

Plerixafor-d4
Plerixafor-d₄ is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].

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

HY-B1456AS

Fenoprofen-13C6(sodium salt hydrate)

Fenoprofen- ¹³C₆ (sodium hydrate) is the ¹³C labeled Fenoprofen (HY-B1456A). Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation[1][2][3].

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-G0021S

N-Desmethylclozapine-d8

N-Desmethylclozapine-d₈ is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].

HY-G0021S1

N-Desmethylclozapine-d8 hydrochloride

N-Desmethylclozapine-d₈ (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].

HY-A0009S

Galanthamine-d3 hydrobromide

Galanthamine-d₃ (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].

HY-10219S1

Rapamycin-13C,d3

Rapamycin- ¹³C,d₃ (Sirolimus- ¹³C,d₃; AY-22989- ¹³C,d₃) is the ¹³C and deuterium labeled Rapamycin (HY-10219) . Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-117287

Deucravacitinib

15+ Cited Publications

Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC₅₀=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .

HY-100386S

Ticlopidine-d4

Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].

HY-113050SA

2,3-Diphosphoglyceric acid-d3 ammonium

2,3-Diphosphoglyceric acid-d3 ammonium (2,3-DPG-d3 ammonium) is the deuterium labeled 2,3-Diphosphoglyceric acid (HY-113050). 2,3-Diphosphoglyceric acid (2,3-DPG) is an intermediate of the glycolytic pathway. 2,3-Diphosphoglyceric acid stabilizes the deoxygenated form of hemoglobin by allosteric binding and facilitates oxygen release at tissue sites. 2, 3-diphosphoglyceric acid has antiparasitic activity. 2,3-Diphosphoglyceric acid can be used in the study of Alzheimer's disease (AD) .

Cat. No.	Product Name		Classification

HY-16062

ARQ 621		Alkynes
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity . ARQ 621 is a kinesin inhibitor . ARQ 621 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-168152

SARS-CoV-2 3CLpro-IN-26		Alkynes
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC₅₀ of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .

HY-118022

VU0361747		Alkynes
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4?PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .

HY-151829

Fmoc-L-Asn(EDA-N3)-OH		Azide
Fmoc-L-Asn(EDA-N3)-OH is a click chemistry reagent containing an azide group. This building block is reported in literature for the modification of Amanitin via Click Chemistry. Alpha-Amanitin is the deadliest member of the amatoxin peptide family produced by the death-cap mushroom A. phalloides. It is an orally available, rigid, bicyclic octapeptide and one of the most lethal known natural products (LD50 = 50-100 μg/kg) acting as highly selective allosteric inhibitor of the RNA polymerase II . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.

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