168 Results for "

ligand-binding

" in MedChemExpress (MCE) Product Catalog:
Products (168)

168 Results for "ligand-binding" in MCE Product Catalog:

50
50 Publications Verification
Cat. No.: HY-13956
CAS No.: 111025-46-8
Purity:  99.89%
Synonyms: U 72107
Target:  

PPAR Ferroptosis

Research Areas:  

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 .
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36
36 Cited Publications
Cat. No.: HY-112288
CAS No.: 432001-19-9
Purity:  99.90%
Synonyms: TTI-101
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
16 Cited Publications
Cat. No.: HY-14422
CAS No.: 1246525-60-9
Purity:  99.75%
Target:  

ROR

Research Areas:  

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 .
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12
12 Cited Publications
Cat. No.: HY-B1322
CAS No.: 6398-98-7
Synonyms: Amodiaquin dihydrochloride dihydrate
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 .
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12
12 Cited Publications
Cat. No.: HY-B1322A
CAS No.: 86-42-0
Synonyms: Amodiaquin
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 .
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12
12 Cited Publications
Cat. No.: HY-B1322B
CAS No.: 69-44-3
Synonyms: Amodiaquin dihydrochloride
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 .
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7
7 Cited Publications
Cat. No.: HY-N0010
CAS No.: 27741-01-1
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 .
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7
7 Cited Publications
Cat. No.: HY-18102
CAS No.: 1215085-92-9
Target:  

Androgen Receptor

Research Areas:  

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 .
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6
6 Cited Publications
Cat. No.: HY-109176
CAS No.: 1953133-47-5
Purity:  99.52%
Synonyms: GDC-9545; RG6171
Target:  

Estrogen Receptor/ERR

Research Areas:  

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 .
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5
5 Cited Publications
Cat. No.: HY-113329
CAS No.: 543-18-0
Purity:  ≥98.0%
Synonyms: Taurocyamine
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 .
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4
4 Cited Publications
Cat. No.: HY-N2025
CAS No.: 57396-78-8
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 .
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3
3 Cited Publications
Cat. No.: HY-P9977
CAS No.: 2171511-58-1
Synonyms: JNJ-61186372

Target:  

EGFR

Research Areas:  

Cancer

Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
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3
3 Cited Publications
Cat. No.: HY-P2264
CAS No.: 676657-00-4
Target:  

Ephrin Receptor

Research Areas:  

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 .
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2
2 Cited Publications
Cat. No.: HY-23999
CAS No.: 4929-23-1
Target:  

LOX-1

Research Areas:  

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 .
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1
1 Cited Publications
Cat. No.: HY-P99446
CAS No.: 845264-92-8
Synonyms: TACI-Ig; TACI-Fc 5

Target:  

TNF Receptor

Research Areas:  

Inflammation/Immunology

Atacicept (TACI-Ig) is a is a recombinant fusion protein containing the extracellular, ligand-binding portion of the TACI receptor and the Fc portion of human IgG. Atacicept inhibits B cell stimulation by binding to B lymphocyte stimulator and a proliferation-inducing ligand. Atacicept can be used in research of B-cell autoimmune disease .
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1
1 Cited Publications
Cat. No.: HY-130714
CAS No.: 2305936-56-3
Purity:  99.41%
Target:  

PROTACs

Research Areas:  

Cancer

TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group .
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1
1 Cited Publications
Cat. No.: HY-N4194
CAS No.: 60008-02-8
Glabrone is an isoflavone found in Glycyrrhiza glabra roots. Glabrone exhibits significant PPAR-γ ligand binding activity. Glabrone is a specific UGT1A9 probe substrate, and its metabolites can block influenza virus release by inhibiting neuraminidase (NA). Glabrone can be used to screen for herb-drug interactions and for anti-influenza virus activity .
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1
1 Cited Publications
Cat. No.: HY-P10579
CAS No.: 2225868-19-7
Target:  

Ephrin Receptor

Research Areas:  

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 .
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1
1 Cited Publications
Cat. No.: HY-135345
CAS No.: 2079056-43-0
Purity:  99.48%
Target:  

PROTACs FKBP

Research Areas:  

Cancer

PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader .
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1
1 Cited Publications
Cat. No.: HY-128838A
Purity:  98.18%
Research Areas:  

Others

(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader .
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