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ligand binding domain

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Epigenetic Reader Domain (2) FKBP (2) Adrenergic Receptor (1) Akt (3) AMPK (1) Androgen Receptor (12) Angiotensin-converting Enzyme (ACE) (2) Antibiotic (1) APC (1) Apoptosis (6) ATF6 (1) Autophagy (1) Calcium Channel (1) Caspase (1) CXCR (1) DNA Methyltransferase (1) EGFR (19) Endogenous Metabolite (4) Environmental Pollutants (1) Ephrin Receptor (2) Estrogen Receptor/ERR (12) Ferroptosis (7) FXR (2) Glutathione Peroxidase (1) Glycosidase (2) Histone Acetyltransferase (1) Histone Methyltransferase (11) IGF-1R (1) iGluR (6) IKZF Family (1) Interleukin Related (2) IRE1 (1) Isotope-Labeled Compounds (3) JAK (1) Ligands for E3 Ligase (4) LOX-1 (1) LXR (2) Mitosis (1) Mixed Lineage Kinase (1) Molecular Glues (1) mTOR (1) Na+/H+ Exchanger (NHE) (1) nAChR (1) Natriuretic Peptide Receptor (NPR) (1) Nuclear Hormone Receptor 4A/NR4A (10) Orphan Nuclear Receptor (3) p62 (1) Parasite (8) PGC-1α (2) Phosphatase (1) PI3K (1) PPAR (11) Pregnane X Receptor (PXR) (1) Prostaglandin Receptor (1) PROTACs (4) RAR/RXR (1) Ras (1) Reactive Oxygen Species (ROS) (2) Reference Standards (6) REV-ERB (1) RIP kinase (1) ROR (2) SARS-CoV (2) Sirtuin (1) Src (1) STAT (1) TGF-β Receptor (1) Thyroid Hormone Receptor (1) TNF Receptor (1) Transmembrane Glycoprotein (2) Trk Receptor (1) TSH Receptor (1) VD/VDR (1) VEGFR (1) Wnt (1)
By Research Areas:	Cancer (69) Cardiovascular Disease (4) Endocrinology (5) Infection (12) Inflammation/Immunology (17) Metabolic Disease (20) Neurological Disease (22)
Click Chemistry:	PROTAC Synthesis (1)

127

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

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Isotope-Labeled Compounds

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Pioglitazone Maximum Cited Publications 47 Publications Verification U 72107	PPAR Ferroptosis	Metabolic Disease Cancer
Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .

Giredestrant 5 Publications Verification GDC-9545; RG6171	Estrogen Receptor/ERR	Cancer
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity .

Shield-1 5+ Cited Publications Shld1	FKBP	Others
Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD) .

SR1078 10+ Cited Publications	ROR	Cancer
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .

Amodiaquine dihydrochloride dihydrate 10+ Cited Publications Amodiaquin dihydrochloride dihydrate	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

Amodiaquine 10+ Cited Publications Amodiaquin	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

Nimotuzumab 1 Publications Verification h-R3	EGFR	Cancer
Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a K_D of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC) .

Teprotumumab 1 Publications Verification	IGF-1R TSH Receptor	Endocrinology
Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research .

Apcin 5+ Cited Publications	APC Mitosis	Cancer
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis .

Ramucirumab (anti-VEGFR) 1 Publications Verification	VEGFR	Cancer
Ramucirumab (anti-VEGFR) is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab (anti-VEGFR) is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab (anti-VEGFR) is also an angiogenesis inhibitor .

BI-0115 2 Publications Verification	LOX-1	Cardiovascular Disease
BI-0115 is a selective inhibitor of LOX-1 (IC₅₀=5.4 μM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain .

APY29 10+ Cited Publications	IRE1	Cancer
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC₅₀ of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .

Amodiaquine dihydrochloride 10+ Cited Publications Amodiaquin dihydrochloride	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a K_i of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

Rilonacept Arcalyst; IL 1 Trap; Interleukin 1 Trap	Interleukin Related	Inflammation/Immunology
Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes .

Anbenitamab 1 Publications Verification KN-026	EGFR	Cancer
Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting extracellular domains II and IV of human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathways. Anbenitamab mediates antibody-dependent cellular cytotoxicity (ADCC) via FcγIIIa binding. Ambrinitumab can be used in research for lung cancer, HER2-positive metastatic breast cancer (MBC), gastric cancer, and gastroesophageal junction cancer .

Oroxin A 4 Publications Verification	PPAR Glycosidase	Metabolic Disease
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .

UNC 669 2 Publications Verification	Epigenetic Reader Domain	Cancer
UNC 669, a ligand for a methyl-lysine binding domain, is a potent L3MBTL1 (IC₅₀=4.2 uM) and L3MBTL3 (3.1 uM) inhibitor .

PF-06273340	Trk Receptor	Neurological Disease
PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC₅₀ values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .

DS45500853	Estrogen Receptor/ERR	Metabolic Disease
DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC₅₀ value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .

UT-34	Estrogen Receptor/ERR	Endocrinology Cancer
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC₅₀ values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.

Vixticibart REGN-5381	Natriuretic Peptide Receptor (NPR)	Cardiovascular Disease
Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension .

VVD-849	Ras PI3K Akt	Cancer
VVD-849 is a RAS ligand. VVD-849 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT (S473) in HER2-overexpressing tumors. VVD-849 can be used for the research of cancers such as breast cancer .

4,8-Dioxa-3H-perfluorononanoic acid	Pregnane X Receptor (PXR)	Endocrinology
4,8-Dioxa-3H-perfluorononanoic acid is an ether-substituted polyfluoroalkyl compound and also a ligand of human pregnane X receptor (hPXR), which binds to the ligand-binding domain of hPXR. 4,8-Dioxa-3H-perfluorononanoic acid targets Arg-410, Lys-210, Lys-226, Met-323 and His-327 residues. Its binding process relies on long-range electrostatic interactions, and no significant hydrogen bonds form with hPXR residues. 4,8-Dioxa-3H-perfluorononanoic acid is used as a substitute for PFOA in Germany. 4,8-Dioxa-3H-perfluorononanoic acid is detectable in environmental matrices such as river water near fluoride production plants, accumulates in organisms including grass, deer liver and locusts, and is present in plasma samples of populations in southern Germany .

GLPG0492 5+ Cited Publications	Androgen Receptor	Neurological Disease
GLPG0492 is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .

EPQpYEEIPIYL 1 Publications Verification	Src	Cancer
EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains .

NV03	Histone Methyltransferase Ligands for E3 Ligase	Cancer
NV03 is a potent and selective antagonist of *Ubiquitin-like with PHD and RING finger domains* 1 (UHRF1*)-H3K9me3 interaction by binding* to UHRF1 tandem tudor domain, with a K_d of 2.4 μM. NV03 is also a ligand for E3 ligase. NV03 can be studied in anticancer research .

LLC0424	PROTACs Histone Methyltransferase	Cancer
LLC0424 is a potent and selective cereblon-based *PROTAC nuclear receptor-binding* SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC₅₀** of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .

123B9 1 Publications Verification	Ephrin Receptor	Cancer
123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a K_d value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .

YTK-105	p62 Autophagy	Cancer
YTK-105 is a p62/ZZ binding domain ligand and Autophagy enhancer. YTK-105 activates p62-dependent selective macroautophagy. YTK-105 serves as an autophagy-targeting ligand (ATL) for synthesizing AUTOTAC degraders .

XY018	ROR	Inflammation/Immunology Cancer
XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC₅₀, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .

DS20362725	Estrogen Receptor/ERR	Metabolic Disease
DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC₅₀ value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .

Nurr1 agonist 2	Nuclear Hormone Receptor 4A/NR4A	Others
Nurr1 agonist 2 (Compound 7) is a Nurr1 agonist (EC₅₀: 0.07 μM). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand binding domain (LBD) with a K_d value of 0.14 μM. Nurr1 agonist 2 increases the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) mRNA expression .

KYL peptide 3 Publications Verification	Ephrin Receptor	Inflammation/Immunology
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC₅₀:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .

BTR2000 TFA	Ligands for E3 Ligase	Others
BTR2000 TFA, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 TFA can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562) .

TR antagonist 2	Thyroid Hormone Receptor	Metabolic Disease
TR antagonist 2 (Compound 10a) is a competitive thyroid hormone receptors (TRα/β) antagonist (IC₅₀=47 nM). TR antagonist 2 competes with triiodothyronine (T₃) for binding to the ligand-binding domain of TR to block receptor-coactivator complex formation and inhibit target gene transcription, reducing thyroid hormone-mediated hypermetabolic effects. TR antagonist 2 is promising for research of hyperthyroidism (e.g., Graves' disease) and thyrotoxicosis .

HD5	SARS-CoV Angiotensin-converting Enzyme (ACE)	Infection Cancer
HD5 is an innate immune effector peptide and SARS-CoV Inhibitor. HD5 binds to the ligand-binding domain of angiotensin-converting enzyme-2 (ACE2) via multiple hydrogen bonds to competitively block the receptor, shielding it from viral recognition. HD5 can be used for the research of COVID-19, HPV16 infection, epithelial ovarian cancer, small-cell lung cancer, and colon cancer .

SR19881	Estrogen Receptor/ERR	Cardiovascular Disease
SR19881 is a potent dual agonist of ERRγ and ERRβ, with EC₅₀ values of 0.39 and 0.63 μM, respectively .

Amodiaquine dihydrochloride dihydrate (Standard) Amodiaquin dihydrochloride dihydrate (Standard)	Nuclear Hormone Receptor 4A/NR4A Reference Standards Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

LYA914	PROTACs Androgen Receptor Akt	Cancer
LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .

LXRβ ligand 1	LXR	Others
LXRβ ligand 1 is a LXR β ligand-binding domain agonist, with an EC₅₀ of 57 μM and a K_i of 28 μM against human LXR β. LXRβ ligand 1 forms hydrogen bonds with His435, stabilizes the His-Trp activation switch, and locks the ligand-binding domain in an agonist conformation; its tert-butyl moiety occupies a hydrophobic subpocket, while its phenyl moiety forms a π-π stacking interaction with Phe329. LXRβ ligand 1 serves as a structural unit for the development of LXRβ modulators .

BTR2000	Ligands for E3 Ligase	Others
BTR2000, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562) .

CBP/p300 ligand 3	Epigenetic Reader Domain Histone Acetyltransferase	Neurological Disease Cancer
CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function .

7α,24(S)-Dihydroxycholesterol (3β,7α,24S)-Cholest-5-ene-3,7,24-triol	Endogenous Metabolite	Others
7α,24(S)-Dihydroxycholesterol ((3β,7α,24S)-Cholest-5-ene-3,7,24-triol) serves as a ligand for liver X receptor (LXR), binding specifically to the ligand binding domains of both LXRα and LXRβ. This compound is synthetically produced from E-α,β-enone, utilizing Arsonium ylide and J-tert-butyldimethylsilyloxy-bisnor-5-cholenaldehyde as starting materials, followed by a series of transformations to yield 7α,24(S)-dihydroxycholesterol.

Nimotuzumab (powder)	EGFR	Cancer
Nimotuzumab (powder) is a humanized IgG1 monoclonal antibody targeting EGFR with a K_D value of 0.21 nM. Nimotuzumab (powder) is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab (powder), a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC) .

GPR110 peptide agonist P12	Transmembrane Glycoprotein	Others Cancer
GPR110 peptide agonist P12 is a peptide that acts as a GPR110 agonist. GPR110 peptide agonist P12 can significantly enhance the initial rate of GPR110 stimulated G protein GTPγS binding. GPR110 peptide agonist P12 mimics the action of natural ligands, causing the extracellular domain (ECD) of the GPR110 to dissociate from the seven transmembrane domains (7TM), exposing the β-strand-13/stalk region at the N-terminus of the 7TM domain, which acts as an agonist to activate G protein signaling. GPR110 peptide agonist P12 can be used in the study of developmental disorders and cancers related to GPR110 .

Cat. No.	Product Name	Target	Research Area

HY-P3279

EPQpYEEIPIYL 1 Publications Verification	Src	Cancer
EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains .

HY-P10579

123B9 1 Publications Verification	Ephrin Receptor	Cancer
123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a K_d value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .

HY-P2264

KYL peptide 3 Publications Verification	Ephrin Receptor	Inflammation/Immunology
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC₅₀:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .

HY-P10495A

GPR110 peptide agonist P12 acetate	Peptides	Cancer
GPR110 peptide agonist P12 acetate is the acetate salt form of GPR110 peptide agonist P12 (HY-P10495). GPR110 peptide agonist P12 acetateis a peptide that acts as a GPR110 agonist. GPR110 peptide agonist P12 acetate can significantly enhance the initial rate of GPR110 stimulated G protein GTPγS binding. GPR110 peptide agonist P12 acetate mimics the action of natural ligands, causing the extracellular domain (ECD) of the GPR110 to dissociate from the seven transmembrane domains (7TM), exposing the β-strand-13/stalk region at the N-terminus of the 7TM domain, which acts as an agonist to activate G protein signaling. GPR110 peptide agonist P12 acetate can be used in the study of developmental disorders and cancers related to GPR110 .

HY-P5407

HD5	SARS-CoV Angiotensin-converting Enzyme (ACE)	Infection Cancer
HD5 is an innate immune effector peptide and SARS-CoV Inhibitor. HD5 binds to the ligand-binding domain of angiotensin-converting enzyme-2 (ACE2) via multiple hydrogen bonds to competitively block the receptor, shielding it from viral recognition. HD5 can be used for the research of COVID-19, HPV16 infection, epithelial ovarian cancer, small-cell lung cancer, and colon cancer .

HY-P10366

WEYIPNV	Peptides	Infection
WEYIPNV is a ligand for SurA, specifically binding to the P1 domain of SurA (K_d: 1-14 μM). The binding of WEYIPNV promotes the release of the P1 domain from the core domain .

HY-P10495

GPR110 peptide agonist P12	Transmembrane Glycoprotein	Others Cancer
GPR110 peptide agonist P12 is a peptide that acts as a GPR110 agonist. GPR110 peptide agonist P12 can significantly enhance the initial rate of GPR110 stimulated G protein GTPγS binding. GPR110 peptide agonist P12 mimics the action of natural ligands, causing the extracellular domain (ECD) of the GPR110 to dissociate from the seven transmembrane domains (7TM), exposing the β-strand-13/stalk region at the N-terminus of the 7TM domain, which acts as an agonist to activate G protein signaling. GPR110 peptide agonist P12 can be used in the study of developmental disorders and cancers related to GPR110 .

HY-P10430

Stalk peptide	Transmembrane Glycoprotein	Neurological Disease
Stalk peptide is a GPR110 activator. Stalk peptide is released from GPCR Autoproteolysis INducing domain by autocatalytic process and then Stalk peptide is inserted into the ligand-binding pocket of the receptor to activate the receptor. Stalk peptide can promote nerve growth and synaptic formation. Stalk peptide can be used to study neurodevelopmental and neurodegenerative diseases .

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-P10671

WVSAV	Phosphatase	Others
WVSAV is a ligand of the PDZ2 domain (Tyrosine Phosphatase) with a K_d value of 111 μM. WVSAV can be used for binding studies in the field of protein-ligand interactions .

HY-P5407A

HD5 TFA	SARS-CoV Angiotensin-converting Enzyme (ACE)	Infection Cancer
HD5 TFA is an innate immune effector peptide and SARS-CoV Inhibitor. HD5 TFA binds to the ligand-binding domain of angiotensin-converting enzyme-2 (ACE2) via multiple hydrogen bonds to competitively block the receptor, shielding it from viral recognition. HD5 TFA can be used for the research of COVID-19, HPV16 infection, epithelial ovarian cancer, small-cell lung cancer, and colon cancer .

Cat. No.	Product Name	Target	Research Area	Image

HY-P9968

Nimotuzumab 1 Publications Verification h-R3	EGFR	Cancer
Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a K_D of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC) .

HY-P99165

Teprotumumab 1 Publications Verification	IGF-1R TSH Receptor	Endocrinology
Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research .

HY-P9920A

Ramucirumab (anti-VEGFR) 1 Publications Verification	VEGFR	Cancer
Ramucirumab (anti-VEGFR) is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab (anti-VEGFR) is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab (anti-VEGFR) is also an angiogenesis inhibitor .

HY-108822

Rilonacept Arcalyst; IL 1 Trap; Interleukin 1 Trap	Interleukin Related	Inflammation/Immunology
Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes .

HY-P99437

Anbenitamab 1 Publications Verification KN-026	EGFR	Cancer
Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting extracellular domains II and IV of human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathways. Anbenitamab mediates antibody-dependent cellular cytotoxicity (ADCC) via FcγIIIa binding. Ambrinitumab can be used in research for lung cancer, HER2-positive metastatic breast cancer (MBC), gastric cancer, and gastroesophageal junction cancer .

HY-P990951

Vixticibart REGN-5381	Natriuretic Peptide Receptor (NPR)	Cardiovascular Disease
Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension .

HY-P9968A

Nimotuzumab (powder)	EGFR	Cancer
Nimotuzumab (powder) is a humanized IgG1 monoclonal antibody targeting EGFR with a K_D value of 0.21 nM. Nimotuzumab (powder) is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab (powder), a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC) .

HY-P991781

Anti-Mouse CXCR6 Antibody (Cx6Mab-1)	CXCR	Inflammation/Immunology
Anti-Mouse CXCR6 Antibody (Cx6Mab-1) reacts with the N-terminal extracellular ligand-binding domain of mouse CXCR6. Recommend Isotype Controls: Rat IgG1 kappa, Isotype Control (HY-P99979) .

HY-P991855

RKER-216	TGF-β Receptor	Metabolic Disease
RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a K_D of 58.7 pM. RKER-216 reduces hepcidin transcription in Hep3B.RKER-216 competes with BMP ligands for binding to the extracellular domain of ALK2, thereby inhibiting BMP-SMAD signal. RKER-216 mobilizes tissue iron effectively in inflammatory conditions. RKER-216 improves microcytic anemia in a dose-dependent manner by inhibiting SMAD signaling to reduce hepcidin and promote iron absorption and utilization in vivo. RKER-216 can be used for research on anemia of inflammation .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113329

Guanidinoethyl sulfonate 5 Publications Verification Taurocyamine	Natural Products Other disease Classification of Application Fields Disease markers Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC₅₀=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABA_A receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .

HY-N0010

Geniposidic acid Maximum Cited Publications 7 Publications Verification	Structural Classification other families Iridoids Classification of Application Fields Terpenoids Plants Endogenous metabolite Disease Research Fields Source Classification Cancer	FXR Sirtuin TNF Receptor Interleukin Related
Geniposidic acid is an orally active FXR modulator and SIRT6 activator. Geniposidic acid binds to the Ser332 and His447 sites on the FXR ligand-binding domain, thereby driving nuclear translocation, coactivator recruitment, and transcription of downstream bile acid and cholesterol metabolism-related genes. Geniposidic acid improves metabolic dysfunction-related fatty liver disease by activating the SIRT6 signaling pathway. Geniposidic acid inhibits inflammation and modulates gut microbiota to alleviate colitis. Geniposidic acid can be used in research on drug-induced liver injury, inflammatory bowel disease, metabolic dysfunction-related fatty liver disease, and metabolic dysfunction-related steatohepatitis .

HY-W017113

2-Mercaptobenzothiazole 1 Publications Verification	Structural Classification Natural Products Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Environmental Pollutants Endogenous Metabolite
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC₅₀ value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .

HY-N2025

Oroxin A 4 Publications Verification	Flavonoids Classification of Application Fields Flavones Metabolic Disease Bignoniaceae Plants Oroxylum indicum (Linn.) Bentham ex Kurz Disease Research Fields Source Classification	PPAR Glycosidase
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .

HY-113329R

Guanidinoethyl sulfonate (Standard) Taurocyamine (Standard)	Structural Classification Natural Products Other disease Disease markers Endogenous metabolite	Endogenous Metabolite Reference Standards
Guanidinoethyl sulfonate (Standard) is the analytical standard of Guanidinoethyl sulfonate. This product is intended for research and analytical applications. Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .

HY-13956R

Pioglitazone (Standard) U 72107 (Standard)	Human Gut Microbiota Metabolites Endogenous metabolite Source Classification	Reference Standards PPAR Ferroptosis
Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .

HY-N2025R

Oroxin A (Standard)	Structural Classification Flavonoids Flavones Bignoniaceae Plants Oroxylum indicum (Linn.) Bentham ex Kurz Source Classification	Reference Standards PPAR Glycosidase
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .

Cat. No.	Product Name	Chemical Structure

HY-13956S1

Pioglitazone-d4 (alkyl)
Pioglitazone-d₄ (alkyl) (U 72107-d₄ (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively .

HY-B1322AS

Amodiaquine-d10
Amodiaquine-d₁₀ is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-13956S

Pioglitazone-d4
Pioglitazone-d₄ is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively .

HY-B1322AS1

Amodiaquine-d10 hydrochloride
Amodiaquine-d₁₀ hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-18102BS

GLPG0492-13C,d3 racemate

GLPG0492- ¹³C,d₃ racemate is ¹³C-labeled GLPG0492 (racemate) (HY-18102B). GLPG0492 racemate is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 racemate exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 racemate effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 racemate prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .

Cat. No.	Product Name		Classification

HY-114402

ARD-69		PROTAC Synthesis
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

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