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ligand-binding domain

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13956
    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 .
    Pioglitazone
  • HY-109176
    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 .
    Giredestrant
  • HY-14422
    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 .
    SR1078
  • HY-B1322
    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 dihydrochloride dihydrate
  • HY-113329
    Guanidinoethyl sulfonate
    5 Publications Verification

    Taurocyamine

    		 Endogenous Metabolite Metabolic Disease
    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 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 .
    Guanidinoethyl sulfonate
  • HY-B1322A
    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 .
    Amodiaquine
  • 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 .
    Teprotumumab
  • HY-N0010
    Geniposidic acid
    Maximum Cited Publications
    7 Publications Verification

    		 FXR Sirtuin TNF Receptor Interleukin Related Metabolic Disease
    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 .
    Geniposidic acid
  • HY-P2917
    Glycerol kinase, microorganism

    GyK

    		 Nuclear Hormone Receptor 4A/NR4A Metabolic Disease Inflammation/Immunology
    Glycerol kinase, microorganism (GyK) acts as a NR4A1 inhibitor with enzymatic activity. It directly binds to and inhibits the transcription factor NR4A1, thereby negatively regulating hepatic gluconeogenesis and reducing blood glucose levels. Glycerol kinase, microorganism positively regulates UCP1 expression via partial dependence on the β-adrenergic receptor-cAMP-CREB pathway, promotes browning of white adipose tissue and thermogenesis, and further modulates intracellular fatty acid composition and energy metabolism. In diabetic mouse models, overexpression of Glycerol kinase effectively antagonizes NR4A1-induced hyperglycemia, demonstrating potential for improving glucose homeostasis. Glycerol kinase, microorganism can be used for studies on diabetes and obesity .
    Glycerol kinase, microorganism
  • HY-W017113
    2-Mercaptobenzothiazole
    1 Publications Verification

    		 Environmental Pollutants Endogenous Metabolite Metabolic Disease
    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 .
    2-Mercaptobenzothiazole
  • HY-23999
    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 .
    BI-0115
  • HY-B1322B
    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 Ki 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 .
    Amodiaquine dihydrochloride
  • 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 .
    Rilonacept
  • HY-N2025
    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 .
    Oroxin A
  • HY-136242
    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.
    UT-34
  • HY-132205
    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) .
    DS45500853
  • HY-W073128
    Perfluorotetradecanoic acid

    PFTeDA

    		 PPAR Apoptosis PGC-1α AMPK Akt mTOR Reactive Oxygen Species (ROS) Endocrinology
    Perfluorotetradecanoic acid (PFTeDA) is an orally active perfluoroalkyl substance. Perfluorotetradecanoic acid directly binds to the ligand-binding domain of purified hPPARγ, with a Kd value of 157.8 μM. Perfluorotetradecanoic acid significantly reduces the activity of the SIRT1/PGC1α and AMPK signaling pathways while stimulating the activity of the AKT1/mTOR signaling pathway. Perfluorotetradecanoic acid significantly upregulates the expression of corticosterone biosynthesis genes. Perfluorotetradecanoic acid increases ROS levels and promotes Apoptosis. Perfluorotetradecanoic acid impairs Leydig cell function and male reproductive endocrine function in adult male rats .
    Perfluorotetradecanoic acid
  • HY-122616
    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 .
    PF-06273340
  • 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 .
    Vixticibart
  • HY-114402
    ARD-69

    		PROTACs Androgen Receptor Cancer
    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).
    ARD-69
  • HY-156190A
    NR2F2-IN-1 free base

    		Orphan Nuclear Receptor Cancer
    NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1 free base
  • HY-18102
    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 .
    GLPG0492
  • HY-W587839
    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 .
    4,8-Dioxa-3H-perfluorononanoic acid
  • HY-P10579
    123B9
    1 Publications Verification

    		 Ephrin Receptor Cancer
    123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd 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 .
    123B9
  • 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 .
    KYL peptide
  • HY-143201
    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) .
    DS20362725
  • HY-122742
    HBT1

    		iGluR Neurological Disease
    HBT1 is an effective AMPA receptor AMPA-R potentiator. HBT1 specifically binds to the ligand-binding domain (LBD) of AMPAR and enhances receptor activity only when AMPA is present., HBT1 has almost no agonistic effect (i.e., reaching the optimal concentration, and then the efficacy decreases as the concentration continues to increase) compared with traditional AMPA-R potentiator, avoiding the bell-shaped reaction of brain-derived neurotrophic factor (BDNF) production in primary neurons. HBT1 can be applicable to a wider range of neurological and psychiatric diseases (such as depression, Alzheimer's disease, etc.) .
    HBT1
  • HY-120210
    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) .
    XY018
  • HY-W677684
    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 Kd 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 .
    Nurr1 agonist 2
  • HY-127024A
    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 .
    TR antagonist 2
  • 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 .
    HD5
  • HY-164552
    ZNU-IMB-Z15

    		Apoptosis Androgen Receptor Cancer
    ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .
    ZNU-IMB-Z15
  • HY-164373
    SC428

    		Androgen Receptor Apoptosis Cancer
    SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
    SC428
  • HY-13956S1
    Pioglitazone-d4 (alkyl)

    		Isotope-Labeled Compounds PPAR Ferroptosis Metabolic Disease Cancer
    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 .
    Pioglitazone-d4 (alkyl)
  • HY-156190
    NR2F2-IN-1

    		Orphan Nuclear Receptor Cancer
    NR2F2-IN-1 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 substantially inhibits COUP-TFII-driven NGFIA reporter expression. NR2F2-IN-1 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1
  • HY-B1322R
    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 .
    Amodiaquine dihydrochloride dihydrate (Standard)
  • HY-113329R
    Guanidinoethyl sulfonate (Standard)

    Taurocyamine (Standard)

    		 Endogenous Metabolite Reference Standards Metabolic Disease
    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 .
    Guanidinoethyl sulfonate (Standard)
  • HY-33821
    LXRβ ligand 1

    		LXR Others
    LXRβ ligand 1 is a LXR β ligand-binding domain agonist, with an EC50 of 57 μM and a Ki 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 .
    LXRβ ligand 1
  • HY-13956B
    Pioglitazone potassium

    U 72107 potassium

    		 PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone (U 72107) potassium 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 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .
    Pioglitazone potassium
  • HY-13956R
    Pioglitazone (Standard)

    U 72107 (Standard)

    		 Reference Standards PPAR Ferroptosis Metabolic Disease Cancer
    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 .
    Pioglitazone (Standard)
  • HY-133830
    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.
    7α,24(S)-Dihydroxycholesterol
  • HY-157281
    Photolumazine III

    PLIII

    		 Endogenous Metabolite Drug Derivative MHC Inflammation/Immunology
    Photolumazine III (PLIII) is a microbial metabolite and derivative of Riboflavin (HY-B0456). Photolumazine III binds MR1 with high specificity. Photolumazine III supports efficient TCR binding. Photolumazine III acts as an antigen to activate cells. Responses to Photolumazine III trigger immune reactions .
    Photolumazine III
  • 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 .
    Stalk peptide
  • HY-13956S
    Pioglitazone-d4

    U 72107-d4

    		 PPAR Ferroptosis Metabolic Disease Cancer
    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 .
    Pioglitazone-d4
  • HY-178938
    AR Degrader-3

    		Molecular Glues Androgen Receptor Caspase Apoptosis Endocrinology Cancer
    AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC) .
    AR Degrader-3
  • HY-110392
    CMP8

    		Estrogen Receptor/ERR Cancer
    CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively .
    CMP8
  • HY-135903
    Giredestrant tartrate

    GDC-9545 tartrate; RG6171 tartrate

    		 Estrogen Receptor/ERR Cancer
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity .
    Giredestrant tartrate
  • HY-113646
    Shield-2

    		FKBP Others
    Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .
    Shield-2
  • HY-13956C
    (R)-Pioglitazone

    (R)-U 72107

    		 PPAR Neurological Disease
    (R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease .
    (R)-Pioglitazone
  • HY-B1322AS
    Amodiaquine-d10

    		Parasite Histone Methyltransferase Infection Neurological Disease Inflammation/Immunology
    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 .
    Amodiaquine-d10

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