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orthosteric inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) ATF6 (1) Caspase (1) Choline Kinase (1) Cyclic GMP-AMP Synthase (2) Dopamine Transporter (1) Enterovirus (1) ERK (1) GABA Receptor (1) GPR84 (1) IFNAR (2) IKK (1) Integrin (1) Interleukin Related (2) JAK (1) mAChR (1) mGluR (1) mTOR (1) PANK (1) Prostaglandin Receptor (1) RAD51 (1) Raf (2) Ras (2) SARS-CoV (1) Sodium Channel (1) Succinate Receptor 1 (1) Tau Protein (1) Toll-like Receptor (TLR) (2) Virus Protease (1)
By Research Areas:	Cancer (6) Cardiovascular Disease (2) Infection (1) Inflammation/Immunology (5) Neurological Disease (11)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-124634

PZ-2891 4 Publications Verification	PANK	Neurological Disease
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC₅₀s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .

HY-175552

CHIPOpt	Tau Protein	Neurological Disease
CHIPOpt, a peptide, is an orthosteric CHIP TPR domain inhibitor with a K_d of ∼16 nM. CHIPOpt has anti-aggregation activity and decreases p.tau ubiquitination with little effect on unmodified tau. CHIPOpt can be used for Alzheimer’s disease research .

HY-150147

CAM833 1 Publications Verification	RAD51 Apoptosis	Cancer
CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a K_d of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis .

HY-174801

XL-3156	Cyclic GMP-AMP Synthase	Inflammation/Immunology
XL-3156 is a cGAS inhibitor. XL-3156 occupies both allosteric and orthosteric sites simultaneously, and inhibits the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of diseases such as autoimmune diseases and inflammation .

HY-159829

Direclidine NBI-1117568; HTL-0016878	mAChR	Neurological Disease
Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .

HY-126242S

Tyk2-IN-7	JAK IFNAR Interleukin Related	Inflammation/Immunology
Tyk2-IN-7 is an orally active TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC₅₀ and K_i.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 can inhibit the IL-23 and IFN-α signaling pathways. Tyk2-IN-7 is commonly used in the study of inflammatory conditions such as colitis .

HY-N1910

4'-O-Methylbavachalcone 4 Publications Verification	SARS-CoV Virus Protease Succinate Receptor 1 ERK	Infection Neurological Disease
4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC₅₀ of 10.1 μM and a K_i of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy .

HY-176487

SARM1-IN-6	Toll-like Receptor (TLR)	Neurological Disease
SARM1-IN-6 (Compound 22b) is a brain-permeable SARM1 orthosteric inhibitor, the IC₅₀ of SARM1-IN-6 against NAM is 0.069 μM .

HY-117764

LSP4-2022	mGluR	Neurological Disease
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC₅₀ of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .

HY-176550

ASIC1a antagonist-1	Sodium Channel	Neurological Disease
ASIC1a antagonist-1 (Compound 5b) is an orthosteric noncompetitive Acid sensing ion channels 1a (ASIC1a) antagonist with an IC₅₀ of 27 nM (pH 6.7). ASIC1a antagonist-1 shifts pH dependence of ASIC1a activation and inhibits its maximal evoked response. ASIC1a antagonist-1 completely inhibits long-term potentiation (LTP) induction in CA3-CA1 pathway. ASIC1a antagonist-1 can be used for brain diseases and pathologies research .

HY-174802

XL-3158	Cyclic GMP-AMP Synthase IKK IFNAR	Neurological Disease Inflammation/Immunology Cancer
XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC₅₀: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.

HY-170805

UNC0737	Choline Kinase	Cancer
UNC0737 is an orthosteric choline kinase inhibitor. UNC0737 is also a poor inhibitor of G9a (IC₅₀ = 5000 nM) and GLP (IC₅₀ > 10000 nM) in the SAHH-coupled assays .

HY-176783

GNE-5152	Toll-like Receptor (TLR)	Neurological Disease
GNE-5152 is an orthosteric SARM1 base-exchange (BE) inhibitor. GNE-5152 sustainably activates SARM1 at subinhibitory concentrations under mildly activating conditions, and this synergistic adverse effect increases NAD consumption, induces axon degradation and neurodegeneration and releases neurofilament-light (NfL) in cortical neurons. GNE-5152 can be used for neurodegenerative diseases research .

HY-P10051

Cyclorasin 9A5	Ras Raf	Cancer
Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC₅₀ of 120 nM .

HY-120694

ML165 RUC-2	Integrin	Cardiovascular Disease
ML165 (RUC-2) is an aIIbb3 receptor antagonist. ML165 has orthosteric inhibition effect at the RGD binding domain. ML165 inhibits platelet adhesion to fibrinogen, and inhibits platelet aggregation (IC₅₀: 96 nM) .

HY-158104

LPPM-8	ATF6	Others
LPPM-8 is a ligand of Med25 and an inhibitor of Med25 protein-protein interactions (PPIs). LPPM-8 engages Med25 through interaction with the H2 face of its Activator Interaction Domain and stabilizes full-length protein in the cellular proteome. LPPM-8 is an orthosteric inhibitor of H2-binding transcriptional activators (such as ATF6a). LPPM-8 can be used for studying Med25 and Mediator complex biology .

HY-P10051A

Cyclorasin 9A5 TFA	Ras Raf	Cancer
Cyclorasin 9A5 TFA is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC₅₀ of 120 nM .

HY-142972

19(S)-HETE	Prostaglandin Receptor	Cardiovascular Disease
19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC₅₀ value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels .

HY-174147

GABAB receptor antagonist 4	GABA Receptor	Neurological Disease
GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist. GABAB receptor antagonist 4 can inhibit GABA-induced G protein activation. GABAB receptor antagonist 4 competitively binds to the orthosteric site of GABAB receptor. GABAB receptor antagonist 4 can be used to study GABAB receptor-related neurological diseases .

HY-172660

36R-D481	Interleukin Related	Inflammation/Immunology
36R-D481 is a competitive and orthosteric antagonist of IL-36R, effectively inhibiting IL-36 signaling. 36R-D481 can inhibit IL-36α and IL-36γ but not IL-36β induced IL-8 release .

HY-179714

DAM-001 Z236004662	Dopamine Transporter	Neurological Disease
DAM-001 (Z236004662) is a potent, non-competitive allosteric inhibitor for human dopamine transporter (hDAT) with an IC₅₀ of 24.70 μM and 1.026 μM in the absence and presence of orthosteric inhibitor Nomifensine (HY-B1110) .

HY-182921

GPR84 antagonist 11	GPR84 Enterovirus	Inflammation/Immunology
GPR84 antagonist 11 is a highly selective GPR84 antagonist, with a human pA₂ of 8.41 and a pK_i of 8.16. GPR84 antagonist 11 competitively inhibits the binding of agonists to the orthosteric site of GPR84 and has improved druglike properties, though its metabolic stability still requires optimization. GPR84 antagonist 11 can be used in the research of autoimmune diseases and fibrotic diseases .

HY-150108

RMC-4745	mTOR Apoptosis Caspase	Cancer
RMC-4745 is a selective dual-site inhibitor of mTORC1, with a selectivity of 35 times for mTORC1 and mTORC2. RMC-4745 inhibits the proliferation of MCF-7 cells and upregulates Caspase-3/7 activity to induce cell apoptosis. RMC-4745 does not cause the upregulation of HER3 due to the inhibition of mTORC2. RMC-4745 can be used for the study of breast cancer .

Cat. No.	Product Name	Target	Research Area

HY-175552

CHIPOpt	Tau Protein	Neurological Disease
CHIPOpt, a peptide, is an orthosteric CHIP TPR domain inhibitor with a K_d of ∼16 nM. CHIPOpt has anti-aggregation activity and decreases p.tau ubiquitination with little effect on unmodified tau. CHIPOpt can be used for Alzheimer’s disease research .

HY-P10051

Cyclorasin 9A5	Ras Raf	Cancer
Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC₅₀ of 120 nM .

HY-158104

LPPM-8	ATF6	Others
LPPM-8 is a ligand of Med25 and an inhibitor of Med25 protein-protein interactions (PPIs). LPPM-8 engages Med25 through interaction with the H2 face of its Activator Interaction Domain and stabilizes full-length protein in the cellular proteome. LPPM-8 is an orthosteric inhibitor of H2-binding transcriptional activators (such as ATF6a). LPPM-8 can be used for studying Med25 and Mediator complex biology .

HY-P10051A

Cyclorasin 9A5 TFA	Ras Raf	Cancer
Cyclorasin 9A5 TFA is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC₅₀ of 120 nM .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1910

4'-O-Methylbavachalcone 4 Publications Verification	Infection Structural Classification Chalcones Flavonoids Classification of Application Fields Leguminosae Phenols Polyphenols Psoralea corylifolia L. Plants Disease Research Fields Source Classification	SARS-CoV Virus Protease Succinate Receptor 1 ERK
4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC₅₀ of 10.1 μM and a K_i of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy .

Cat. No.	Product Name	Chemical Structure

HY-126242S

Tyk2-IN-7
Tyk2-IN-7 is an orally active TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC₅₀ and K_i.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 can inhibit the IL-23 and IFN-α signaling pathways. Tyk2-IN-7 is commonly used in the study of inflammatory conditions such as colitis .

Tyk2-IN-7

Tyk2-IN-7 is an orally active TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC₅₀ and K_i.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 can inhibit the IL-23 and IFN-α signaling pathways. Tyk2-IN-7 is commonly used in the study of inflammatory conditions such as colitis .

Cat. No.	Product Name		Classification

HY-174147

GABAB receptor antagonist 4		Azide
GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist. GABAB receptor antagonist 4 can inhibit GABA-induced G protein activation. GABAB receptor antagonist 4 competitively binds to the orthosteric site of GABAB receptor. GABAB receptor antagonist 4 can be used to study GABAB receptor-related neurological diseases .

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orthosteric inhibitor

Inhibitors & Agonists

Peptides

NaturalProducts

Isotope-Labeled Compounds

Click Chemistry

Natural
Products