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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
103 Results for "
ligand-binding domain
" in MedChemExpress (MCE) Product Catalog:
Products (103)
103 Results for "ligand-binding domain" in MCE Product Catalog:
50
50 Publications Verification
Synonyms: U 72107
Target:
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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 .
36
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C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia .
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16 Cited Publications
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 .
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12 Cited Publications
Synonyms: Amodiaquin dihydrochloride dihydrate
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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 .
12
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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 .
12
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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 .
7
7 Cited Publications
Cat. No.: HY-N0010
CAS No.: 27741-01-1
Category:
other families Iridoids Terpenoids Plants Endogenous metabolite Disease Research Fields Cancer
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7
7 Cited Publications
Cat. No.: HY-18102
CAS No.: 1215085-92-9
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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 .
5
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Natural Products Other disease Disease markers Metabolic Disease Endogenous metabolite Disease Research Fields
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4 Cited Publications
Cat. No.: HY-N2025
CAS No.: 57396-78-8
Category:
Flavonoids Flavones Metabolic Disease Plants Bignoniaceae Oroxylum indicum (Linn.) Bentham ex Kurz Disease Research Fields
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3
3 Cited Publications
Cat. No.: HY-P2264
CAS No.: 676657-00-4
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2
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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 .
1
1 Cited Publications
Cat. No.: HY-P99165
CAS No.: 1036734-93-6
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1
1 Cited Publications
Cat. No.: HY-P10579
CAS No.: 2225868-19-7
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1
1 Cited Publications
Cat. No.: HY-W017113
CAS No.: 149-30-4
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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 .
Synonyms: Arcalyst; IL 1 Trap; Interleukin 1 Trap
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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.
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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) .
Cat. No.: HY-W073128
CAS No.: 376-06-7
Synonyms: PFTeDA
Research Areas:
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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
