Search Result
Results for "
Thyroid Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1
Bibliotecas de Screening
6
Isotope-Labeled Compounds
| Cat. No. |
Nombre del producto |
Target |
Áreas de investigación |
Chemical Structure |
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- HY-13653
-
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EGCG; Epigallocatechol Gallate
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Endogenous Metabolite
Apoptosis
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Inflammation/Immunology
Cancer
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(-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
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-
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- HY-N6791
-
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PKA
PKC
Bacterial
Apoptosis
Antibiotic
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Infection
Inflammation/Immunology
|
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KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a Staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation .
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-
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- HY-13817
-
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Deubiquitinase
Autophagy
Apoptosis
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Cardiovascular Disease
Neurological Disease
Endocrinology
Cancer
|
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IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
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-
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- HY-P99165
-
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IGF-1R
TSH Receptor
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Endocrinology
|
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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 .
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-
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- HY-B1201
-
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3,3',5-Triiodothyroacetic acid
|
Flavivirus
Thyroid Hormone Receptor
TNF Receptor
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Endocrinology
|
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Tiratricol is an orally available thyroid hormone analog that inhibits pituitary thyroid-stimulating hormone secretion. Tiratricol is an intracellular toxin neutralizer that inhibits LPS and lipid A cytotoxicity with IC50s of 20 μM and 32 μM, respectively. Tiratricol reduces TNF production in lipopolysaccharide-stimulated macrophages. Tiratricol also has antiviral activity and is an inhibitor of yellow fever virus (Flavivirus). It can bind to the RdRp domain of the viral NS5 protein to hinder YFV replication. .
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-
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- HY-141513
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NH-3
4 Publications Verification
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Thyroid Hormone Receptor
|
Neurological Disease
|
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NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC50 of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment . NH-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
-
- HY-P99160
-
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hMN14
|
Transmembrane Glycoprotein
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Cancer
|
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Labetuzumab is a humanised anti-carcinoembryonic antigen (CEA) monoclonal antibody that inhibits tumour growth and sensitises human medullary thyroid cancer xenografts to Dacarbazine chemotherapy .
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-
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- HY-115686
-
|
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Adenosine Deaminase
|
Inflammation/Immunology
Cancer
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8-Azaadenosine is a potent ADAR1 inhibitor and an A-to-I editing inhibitor. 8-Azaadenosine blocks RNA editing and inhibits proliferation, 3D growth, invasion, and migration in thyroid cancer cells .
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-
-
- HY-N6033
-
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(+)-Ferruginol
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EBV
HSV
Apoptosis
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Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
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Ferruginol ((+)-Ferruginol), a natural diterpenoid, is an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). Ferruginol inhibits the growth of thyroid cancer cells through the induction of mitochondrial apoptosis. Ferruginol has antitumor, cardioprotective, antioxidant, gastroprotective, and neuroprotective activities .
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-
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- HY-142870
-
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Pyruvate Carboxylase (PC)
Apoptosis
β-catenin
ERK
Wnt
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Cancer
|
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ZY-444 is an anti-cancer agent, targeting pyruvate carboxylase (PC). ZY-444 suppresses the Wnt/β-catenin/Snail signaling pathway by blocking nuclear translocation of β-catenin. ZY-444 selectively inhibits proliferation, migration, and invasion and induces apoptosis in cancer cells. ZY-444 exhibits potent anti-tumor in cancer mouse models. ZY-444 can be used for the study of breast cancer, lung cancer (NSCLC), prostate cancer and iodine-refractory thyroid cancer .
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-
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- HY-B1234
-
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Octyl methoxycinnamate
|
Environmental Pollutants
Estrogen Receptor/ERR
Androgen Receptor
Cytochrome P450
Thyroid Hormone Receptor
|
Metabolic Disease
Endocrinology
|
|
Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
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-
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- HY-W017113
-
|
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Environmental Pollutants
Endogenous Metabolite
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Metabolic Disease
|
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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 .
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-
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- HY-119459
-
-
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- HY-N0526
-
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Sirtuin
Keap1-Nrf2
NF-κB
ERK
p38 MAPK
JNK
TSH Receptor
Reactive Oxygen Species (ROS)
SOD
|
Neurological Disease
Inflammation/Immunology
|
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2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease .
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-
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- HY-W010696
-
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3′,5′,3-Triiodothyronine
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Thyroid Hormone Receptor
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Cardiovascular Disease
|
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Reverse T3 is a thyroid hormone that can be generated by deiodination of the prohormone thyroxine . Reverse T3 inhibits the increase of sodium current generated by other thyroid hormone analogs in neonatal rat myocytes .
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-
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- HY-N0647
-
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Monocarboxylate Transporter
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Endocrinology
|
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Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM .
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-
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- HY-P99364
-
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Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1
|
VEGFR
Apoptosis
p38 MAPK
Akt
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Endocrinology
Cancer
|
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Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is an IgG1 antibody inhibitor targeting VEGFR-1/FLT1 with anti-tumor activity. By blocking ligand-dependent phosphorylation and downstream signal transduction, Icrucumab reduces the activities of MAPK and Akt in breast cancer xenograft models, inhibits the proliferation and invasion of VEGFR-1-positive tumor cells, and reverses the conversion of M1 macrophages to the pro-tumor M2-like phenotype. Icrucumab also inhibits tumor cell proliferation, promotes apoptosis, and effectively suppresses tumor growth through direct targeting of tumors and host support mechanisms. In addition, Icrucumab exhibits a synergistic effect when combined with chemotherapeutic agents, and it is used in research related to various cancers including advanced solid malignancies, thyroid cancer, melanoma, and lung cancer .
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-
-
- HY-19980A
-
PRIMA-1
2 Publications Verification
NSC-281668
|
Autophagy
MDM-2/p53
Ferroptosis
Apoptosis
|
Cancer
|
|
PRIMA-1 (NSC-281668) is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.
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-
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- HY-W008452
-
|
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Endogenous Metabolite
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Metabolic Disease
|
|
H-Tyr(3-I)-OH is a potent and effective tyrosine hydroxylase inhibitor. H-Tyr(3-I)-OH is an intermediate in the production of thyroid hormones and has a role as a human or mouse metabolite .
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-
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- HY-13653R
-
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EGCG(Standard); Epigallocatechol Gallate (Standard)
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Reference Standards
Endogenous Metabolite
Apoptosis
|
Inflammation/Immunology
Cancer
|
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(-)-Epigallocatechin Gallate (Standard) is the analytical standard of (-)-Epigallocatechin Gallate. This product is intended for research and analytical applications. (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
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-
-
- HY-145581
-
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AZD4831
|
Glutathione Peroxidase
Cytochrome P450
|
Cardiovascular Disease
Inflammation/Immunology
|
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Mitiperstat (AZD4831) is an effective oral inhibitor of myeloperoxidase (MPO). Mitiperstat inhibits MPO and thyroid peroxidase (TPO) with IC50s of 1.5 nM and 0.69 μM. Mitiperstat exhibits a weak inhibitory activity against CYP3A4 with an IC50 of 6 μM. Mitiperstat can reduce inflammation and improve microvascular function, and it can be used in studies related to heart failure, preserved or mildly reduced ejection fraction, non-alcoholic fatty liver disease, and chronic obstructive pulmonary disease .
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-
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- HY-34596
-
|
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Biochemical Assay Reagents
Amyloid-β
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Neurological Disease
Metabolic Disease
|
|
4-Hydroxyindole is a type of hydroxyindole in which the 1H-indole at position 4 is substituted by a hydroxyl group.
4-Hydroxyindole serves as an important raw material or intermediate in the synthesis of pharmaceutical products and industrial polymers.
4-Hydroxyindole inhibits amyloid fibrillization and induces liver function impairment, thyroid abnormalities, and blood glucose fluctuations in mice.
4-Hydroxyindole holds potential for research in neurodegenerative diseases and metabolic disorders .
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-
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- HY-Y0470
-
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Aminourea hydrochloride; Hydrazinecarboxamide hydrochloride
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Monoamine Oxidase
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Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
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Semicarbazide hydrochloride is an orally active urea derivative. Semicarbazide hydrochloride binds to copper or iron in cells. Semicarbazide hydrochloride inhibits the activity of soluble semicarbazide sensitive amine oxidase (SSAO). Semicarbazide hydrochloride damages cartilage, blood vessels, ovaries, testicles, and thyroid follicles .
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-
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- HY-114557
-
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3,5-Diiodo-L-thyronine
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JNK
NF-κB
Sirtuin
PGC-1α
COX
TGF-β Receptor
Collagen
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
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NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity .
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- HY-132846
-
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TAS0953/HM06
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RET
Apoptosis
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Cancer
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Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC50 value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas .
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- HY-124828
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CMLD-2
2 Publications Verification
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HuR
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Cancer
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CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation .
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- HY-P991487
-
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Interleukin Related
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Inflammation/Immunology
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LASN01 is a human IgG1 monoclonal antibody (mAb) targeting IL-11RA. LASN01 inhibits IGF-1 and IL-11-induced hyaluronic acid (HA) release and TGFβ-stimulated procollagen in orbital fibroblasts. LASN01 can be used in thyroid eye disease (TED) research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
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- HY-A0152
-
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D-T4
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Endogenous Metabolite
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Metabolic Disease
|
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D-Thyroxine (D-T4) is an orally active thyroid hormone that inhibits the secretion of TSH. D-Thyroxine can inhibit goiter, promote metamorphosis of tadpoles and influence cholesterol metabolism. D-Thyroxine can be used for the study of hypercholesterolemia .
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- HY-153213
-
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TSH Receptor
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Metabolic Disease
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Org 274179-0 is a potent and allosteric antagonist of thyroid-stimulating hormone (TSH) receptor, with an IC50 of nanomolar concentration. Org 274179-0 completely inhibits TSH (and TSI)-mediated TSH receptor activation with little effect on the potency of TSH. Org 274179-0 can be used for the research of Graves' disease (GD) .
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-
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- HY-W009776
-
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Suberohydroxamic acid; SBHA
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HDAC
Apoptosis
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Cancer
|
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Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively .Suberoyl bis-hydroxamic acid renders MM cells susceptible to apoptosis and facilitates the mitochondrial apoptotic pathways .Suberoyl bis-hydroxamic acid can be used for the study of medullary thyroid carcinoma (MTC) .
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- HY-107615
-
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LPL Receptor
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Cancer
|
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TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened agent targets . TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells .
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-
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- HY-156135
-
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MDM-2/p53
RET
DNA/RNA Synthesis
Apoptosis
Caspase
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Endocrinology
Cancer
|
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NSC194598 is a p53 DNA-binding inhibitor with an IC50 value of 180 nM. NSC194598 inhibits p53 DNA binding and induction of target genesn when p53 is stabilized and activated by irradiation or chemotherapy. NSC194598 can interfere with transcriptional activation of mutated rearranged during transfection (RET) gene, induce apoptosis and G0/G1 phase arrest. NSC194598 can be used for the researches of acute radiation toxicity and medullary thyroid carcinoma .
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- HY-144878
-
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c-Myc
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Cancer
|
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VPC-70619 is a potent N-Myc inhibitor. VPC-70619 blocks the binding of the N-Myc-Max heterocomplex to the DNA E-box and exhibits potent inhibitory activity against N-Myc-dependent cell lines. VPC-70619 can partially reverse paclitaxel (HY-B0015) resistance in cells by reducing MYCN expression. VPC-70619 can be used for cancer research (e.g., neuroblastoma and thyroid cancer) .
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-
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- HY-W011258
-
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L-Tyrosyl-L-phenylalanine
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Xanthine Oxidase
Angiotensin-converting Enzyme (ACE)
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Inflammation/Immunology
Cancer
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H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells .
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-
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- HY-101246
-
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RET
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Cancer
|
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RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
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-
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- HY-12753A
-
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SR35021 hydrochloride
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Thyroid Hormone Receptor
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Cardiovascular Disease
|
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Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
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-
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- HY-139915
-
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Glutathione Peroxidase
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Inflammation/Immunology
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MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation .
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- HY-N10348
-
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Drug Derivative
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Endocrinology
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Progoitrin is a sulfur-containing glucosinolate, as well as a naturally occurring orally active thioglycoside. Progoitrin acts as a hepatotoxin and antithyroid agent. Progoitrin is quantitatively converted to goitrin in vivo, including via a gastrointestinal hydrolysis pathway that does not require exogenous myrosinase, thereby blocking the organification of iodine in the thyroid gland and inhibiting the uptake and accumulation of radioactive iodine. Progoitrin can be used in studies related to Graves' disease .
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-
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- HY-150526
-
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Endogenous Metabolite
Apoptosis
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Inflammation/Immunology
Cancer
|
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EGCG-4″-sulfate is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate sulfate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. EGCG-4″-sulfate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
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-
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- HY-N6841
-
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Glucose-6-Phosphate Isomerase (GPI)
Casein Kinase
Virus Protease
Flavivirus
PI3K
Akt
mTOR
Apoptosis
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Infection
Cancer
|
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Rhodiolin, a flavonoid, is an orally active glucose 6-phosphate isomerase (GPI) inhibitor. Rhodiolin inhibits papillary thyroid cancer (PTC) by targeting glycolysis enzyme glucose 6-phosphate isomerase GPI and suppressing PI3K/AKT/mTOR phosphorylation and induce apoptosis. Rhodiolin as a NS2B-NS3 protease inhibitor can disrupt dengue viral replication. Rhodiolin is also a potential candidate for developing anticancer strategies inhibiting CK1ε kinase. Rhodiolin can be used for the study of anti-tumor and anti-viral .
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-
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- HY-13653S1
-
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EGCG-d4; Epigallocatechol Gallate-d4
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Isotope-Labeled Compounds
Apoptosis
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Inflammation/Immunology
Cancer
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(-)-Epigallocatechin Gallate-d4 (EGCG-d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
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-
-
- HY-120026
-
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KB015
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Thyroid Hormone Receptor
Calcium Channel
Potassium Channel
Sodium Channel
|
Cardiovascular Disease
|
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KB130015 (KB015) is an orally active and potent ThRα and ThRβ (thyroid hormone receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 activates hERG1 channels (EC50 = 12.2 μM) and large-conductance Ca 2+-activated K + (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells. KB130015 has antiarrhythmic properties. KB130015 can be used for the study of cardiovascular disease .
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-
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- HY-N0885
-
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Telobufotoxin; Telocinobufogenin
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JAK
STAT
mTOR
PI3K
Akt
Polo-like Kinase (PLK)
Na+/K+ ATPase
Apoptosis
Bacterial
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Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
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Telocinobufagin (Telobufotoxin; Telocinobufogenin) is an orally active bufadienolide with potential anti-tumor effects. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma, osteosarcoma, thyroid cancer, breast cancer and head and neck squamous cell carcinoma by inhibiting the STAT3, JAK2/STAT3, LARP1-mTOR, PI3K/Akt/Snail and PLK1 pathways, and can also induce tumor cell apoptosis. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Telocinobufagin has a strong cardiac-stimulating effect by inhibiting the activity of Na +/K +-ATPase, and it can promote renal fibrosis. Telocinobufagin demonstrates non-opioid analgesic effects in various acute pain models .
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- HY-153213A
-
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TSH Receptor
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Endocrinology
|
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Org 274178-0 is a selective thyroid-stimulating hormone receptor (TSHR) antagonist with a pIC50 value for TSHR is 5.03. Org 274178-0 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by thyroid-stimulating hormone (TSH) and TSH receptor-stimulating immunoglobulins (TSIs). Org 274178-0 is promising for research of Graves’ disease and Graves’ ophthalmopathy .
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-
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- HY-127024A
-
|
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Thyroid Hormone Receptor
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Metabolic Disease
|
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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 .
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-
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- HY-Q04764
-
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Thyroid Hormone Receptor
Apoptosis
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Cancer
|
|
TI17 is an inhibitor of the thyroid hormone receptor-interacting protein Trip13 and has anticancer activity. TI17 effectively inhibits multiple myeloma (MM) cell proliferation and induces cell cycle arrest and apoptosis. Trip13 is an AAA-ATPase that mediates double-strand break (DSB) repair; TI17 inhibits Trip13 function and increases DNA damage .
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-
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- HY-114411
-
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Estrogen Receptor/ERR
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Cancer
|
|
ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC50 value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer .
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-
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- HY-119459R
-
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Reference Standards
Succinate Dehydrogenase
Fungal
Parasite
Constitutive Androstane Receptor
Caspase
NF-κB
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Infection
Cancer
|
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Fluopyram (Standard) is the analytical standard of Fluopyram (HY-119459). This product is intended for research and analytical applications. Fluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC50 values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic .
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-
-
- HY-122041
-
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|
Apoptosis
Poly(ADP-ribose) Glycohydrolase (PARG)
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Cancer
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|
Ethacridine is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor and an activator of the transcriptional coactivator. Ethacridine induces thyroid cancer cells apoptosis and promotes differentiation in thyroid follicular cells .
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-
-
- HY-W415287
-
-
- HY-172661
-
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|
Thyroid Hormone Receptor
Interleukin Related
LDLR
|
Infection
Metabolic Disease
|
|
KYLO-0603 is an orally active, selective THR-β agonist (EC50 : 31.07 nM). KYLO-0603 has significant activity in lowering serum cholesterol and low-density lipoprotein cholesterol. KYLO-0603 upregulates the expression of THR-regulated genes (including iodothyronine deiodinase 1 (Dio1), malic enzyme 1 (Me1), and thyroid hormone response (Thrsp) gene) and inhibits the expression of inflammatory and fibrotic genes (low-density lipoprotein receptor (LDL-R) gene) by activating THR-β receptors. KYLO-0603 can be used to treat metabolic dysfunction-associated steatohepatitis (MASH) and liver fibrosis research .
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-
- HY-N0224A
-
|
(S)-Goitrin; L-5-Vinyl-2-thiooxazolidone
|
Influenza Virus
|
Metabolic Disease
|
|
Goitrin ((S)-Goitrin), a product of glucosinolate-myrosinase reactions, is a potent inhibitor of thyroid peroxidase. Goitrin can inhibit iodine utilization by the thyroid. Goitrin also exhibits anti-influenza virus (H1N1) activity .
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-
- HY-W010696R
-
|
3′,5′,3-Triiodothyronine (Standard)
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Reference Standards
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
|
Reverse T3 (Standard) is the analytical standard of Reverse T3. This product is intended for research and analytical applications. Reverse T3 is a thyroid hormone that can be generated by deiodination of the prohormone thyroxine . Reverse T3 inhibits the increase of sodium current generated by other thyroid hormone analogs in neonatal rat myocytes .
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-
- HY-B1201R
-
|
3,3',5-Triiodothyroacetic acid (Standard)
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Flavivirus
Thyroid Hormone Receptor
Reference Standards
TNF Receptor
|
Endocrinology
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Tiratricol (Standard) is the analytical standard of Tiratricol. This product is intended for research and analytical applications. Tiratricol is an orally available thyroid hormone analog that inhibits pituitary thyroid-stimulating hormone secretion. Tiratricol is an intracellular toxin neutralizer that inhibits LPS and lipid A cytotoxicity with IC50s of 20 μM and 32 μM, respectively. Tiratricol reduces TNF production in lipopolysaccharide-stimulated macrophages. Tiratricol also has antiviral activity and is an inhibitor of yellow fever virus (Flavivirus). It can bind to the RdRp domain of the viral NS5 protein to hinder YFV replication. .
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-
- HY-14815
-
|
Combretastatin A4 phosphate
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Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Fosbretabulin (Combretastatin A4 phosphate) is a vascular disruptor with antitumor activity against atypical thyroid carcinoma (ATC) cell lines and xenografts. Fosbretabulin inhibits tumor growth by inhibiting microtubule polymerization, inducing apoptosis, and suppressing angiogenesis in tumors .
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-
- HY-124070
-
|
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MDM-2/p53
|
Cancer
|
|
ISA 27 is a small-molecule MDM2-p53 protein-protein interaction inhibitor. ISA 27 inhibits MDM2-mediated p53 ubiquitination and degradation. ISA 27 is promising for research of p53-mutant solid tumors (e.g., thyroid, breast cancer) .
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-
- HY-13752
-
|
|
HSP
|
Cancer
|
|
STA-1474 is an orally active and highly selective HSP90 inhibitor. STA-1474 can trigger tumor cell apoptosis. STA-1474 demonstrates significant antitumor efficacy in spontaneous canine cancer models (e.g., osteosarcoma, thyroid carcinoma). STA-1474 is promising for research of solid tumors (e.g., osteosarcoma, breast cancer) and HSP90-driven cancers .
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-
- HY-125535
-
|
|
AMPK
mTOR
Autophagy
Atg8/LC3
|
Cancer
|
|
OSU-53 is an orally active AMPK activator (EC50: 0.3 μM) and a direct mTOR inhibitor. OSU-53 induces autophagy and increases conversion of LC3 I to LC3 II. OSU-53 also modulates energy homeostasis by suppressing fatty acid biosynthesis and shifting the metabolism to oxidation by up-regulating the expression of PGC1α and NRF-1. OSU-53 has antitumor activity in various tumor models, such as breast cancer and thyroid cancer .
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-
- HY-170017S
-
|
EGCG-d3/d4; Epigallocatechol Gallate-d3/d4
|
Isotope-Labeled Compounds
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
(-)-Epigallocatechin Gallate-d3/d4 (EGCG-d3/d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
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-
- HY-163995
-
|
|
Ferroptosis
Glutathione Peroxidase
|
Cancer
|
|
GPX4-IN-13 (compound 16) is a GPX4 inhibitor with anticancer activity. GPX4-IN-13 reduces thyroid cell proliferation and induces ferroptosis by inhibiting the expression level of GPX4. GPX4-IN-13 inhibits the growth of three thyroid cancer cell lines: N-thy-ori-3-1 (IC50=8.39 μM), MDA-T32 (IC50=10.28 μM) and MDA-T41 (IC50=8.18 μM) .
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-
- HY-B1234S
-
|
|
Cytochrome P450
Thyroid Hormone Receptor
Androgen Receptor
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Metabolic Disease
Endocrinology
|
|
Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
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-
- HY-169153
-
|
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-3 (Compound 33) is a potent and selective cancer osaka thyroid (COT) kinase inhibitor, with an IC50 of 4 nM. Cot inhibitor-3 can be used to prevent inflammation-driven lameness .
|
-
- HY-116701
-
|
|
Thyroid Hormone Receptor
|
Others
|
|
A 274 is an amiodarone analogue that has the activity of inhibiting the binding of T3 to α1- and β1-thyroid hormone receptors in vitro. Its IC50 values for inhibition of α1-T3R and β1-T3R are certain values (depending on the specific experimental results).
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-
- HY-169054
-
|
|
TSH Receptor
|
Cancer
|
|
NCATS-SM4420 (Compound A35) is an orally active thyroid-stimulating hormone receptor (TSHR) ligand that inhibits the proliferation of MDA-T32 and MDA-T85 cells in vitro (IC50 values of 0.71 μM and 0.38 μM, respectively) and suppresses metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds promise for research in the field of thyroid cancer .
|
-
- HY-174993
-
|
|
RET
|
Cancer
|
|
FHND5071 (1H) is a selective inhibitor targeting the RET (rearrangement during transfection) tyrosine kinase. FHND5071 (1H) is promising for research of RET-driven cancers (such as thyroid cancer, lung cancer, etc.) .
|
-
- HY-A0152A
-
|
D-T4 sodium
|
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
|
D-thyroxine (D-T4) sodium is an orally active thyroid hormone that inhibits the secretion of TSH. D-thyroxine sodium can inhibit goiter, promote metamorphosis of tadpoles and influence cholesterol metabolism. D-thyroxine sodium can be used for the study of hypercholesterolemia .
|
-
- HY-164482
-
|
|
RET
|
Cancer
|
|
HG-6-63-01 is a type II RET tyrosine kinase inhibitor (TKI). HG-6-63-01 also inhibits REarranged during Transfection (RET) kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles. HG-6-63-01 impairs phosphorylation and signalling of RET oncogenic mutants. HG-6-63-01 blunts proliferation of RET/C634R and RET/M918T-transformed fibroblasts and of RET mutant thyroid cancer cells, which is promising for research of cancers harboring oncogenic activation of RET .
|
-
- HY-156113
-
|
|
RET
|
Cancer
|
|
RET-IN-25 (compound 6b) is a RET kinase inhibitor with anticancer activity. RET-IN-25 inhibits medullary thyroid carcinoma (MTC) with IC50s of 3.6 μM (3 days) and 3.0 μM (6 days) against TT(C634R) MTC .
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-
- HY-110111A
-
|
|
DNA/RNA Synthesis
|
Others
|
|
T2AA hydrochloride is a non-peptide small molecule PCNA inhibitor T2 amino alcohol (T2AA) that lacks thyroid hormone activity. T2AA hydrochloride inhibits the interaction of PCNA/PIP-box peptide (IC50=~1 μM) and the interaction of PCNA with full-length p21 protein .
|
-
- HY-N0647R
-
|
|
Reference Standards
Monocarboxylate Transporter
|
Endocrinology
|
|
Silychristin (Standard) is the analytical standard of Silychristin. This product is intended for research and analytical applications. Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM .
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-
- HY-A0152R
-
|
D-T4 (Standard)
|
Reference Standards
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Thyroxine (Standard) is the analytical standard of D-Thyroxine (HY-A0152). This product is intended for research and analytical applications. D-Thyroxine (D-T4) is an orally active thyroid hormone that inhibits the secretion of TSH. D-Thyroxine can inhibit goiter, promote metamorphosis of tadpoles and influence cholesterol metabolism. D-Thyroxine can be used for the study of hypercholesterolemia .
|
-
- HY-12753AR
-
|
SR35021 hydrochloride (Standard)
|
Reference Standards
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
|
Debutyldronedarone (hydrochloride) (Standard) is the analytical standard of Debutyldronedarone (hydrochloride). This product is intended for research and analytical applications. Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
|
-
- HY-12753AS
-
|
SR35021-d7 hydrochloride
|
Thyroid Hormone Receptor
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Debutyldronedarone-d7 hydrochloride is deuterated labeled Debutyldronedarone hydrochloride (HY-12753A). Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
|
-
- HY-Y0470R
-
|
Aminourea hydrochloride (Standard); Hydrazinecarboxamide hydrochloride (Standard)
|
Antibiotic
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
Semicarbazide (hydrochloride) (Standard) is the analytical standard of Semicarbazide (hydrochloride). This product is intended for research and analytical applications. Semicarbazide hydrochloride is an orally active urea derivative. Semicarbazide hydrochloride binds to copper or iron in cells. Semicarbazide hydrochloride inhibits the activity of soluble semicarbazide sensitive amine oxidase (SSAO). Semicarbazide hydrochloride damages cartilage, blood vessels, ovaries, testicles, and thyroid follicles .
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-
- HY-W008452S
-
-
- HY-164549
-
|
|
RET
|
Cancer
|
XMD15-44 is a RET kinase inhibitor.XMD15-44 has a growth-inhibitory effect on RET/C634R and RET/M918T transformed RAT1 cells, with IC50 values of 11.5 nM and 8.3 nM, respectively. XMD15-44 can inhibit RET kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles, reducing cell proliferation .
|
-
- HY-143546
-
|
|
RET
|
Cancer
|
|
RET-IN-9 is a potent inhibitor of RET. RET kinase is a single-pass transmembrane receptor tyrosine kinase that plays an important role in the development of the kidney and enteric nervous system, and the maintenance of homeostasis in the nervous, endocrine, hematopoietic, and male reproductive systems. RET-IN-9 has the potential for the research of RET-related disease including non-small cell lung cancer and medullary thyroid cancer (extracted from patent WO2021115457A1, compound 29) .
|
-
- HY-114557R
-
|
3,5-Diiodo-L-thyronine (Standard)
|
Reference Standards
Endogenous Metabolite
|
Metabolic Disease
|
|
NSC 90469 (Standard) is the analytical standard of NSC 90469. This product is intended for research and analytical applications. NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity .
|
-
- HY-175302
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
|
TRK-IN-32 is a potent TRK inhibitor. TRK-IN-32 potently inhibits TRK WT, TRK G595R and TRK G667C with IC50 values of 0.08 nM, 2.14 nM and 0.68 nM, respectively. TRK-IN-32 also demonstrates antiproliferative activity against a panel of Ba/F3 cell lines transformed with wild type, xDFG, solvent-front as well as gatekeeper mutant TRK fusion proteins. TRK-IN-32 induces apoptosis of Ba/F3-TRKA WT and Ba/F3-TRKA G667C cells.TRK-IN-32 can be used for the study of various cancers (such as thyroid cancer, secretory breast carcinoma) .
|
-
- HY-N0526R
-
|
|
Reference Standards
Sirtuin
Keap1-Nrf2
NF-κB
ERK
p38 MAPK
JNK
TSH Receptor
Reactive Oxygen Species (ROS)
SOD
|
Neurological Disease
Inflammation/Immunology
|
|
2"-O-Galloylhyperin (Standard) is the analytical standard of 2"-O-Galloylhyperin (HY-N0526). This product is intended for research and analytical applications. 2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease .
|
-
- HY-W713284
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
Estrogen Receptor/ERR
Androgen Receptor
Thyroid Hormone Receptor
|
Endocrinology
|
|
2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
|
-
- HY-177011
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRγ-IN-1 is a ERRγ inhibitor with an IC50 of 0.040 μM. ERRγ-IN-1 activates MAPK (p44/p42) and inhibits the activity of ERRγ. ERRγ-IN-1 significantly increases iodine uptake in anaplastic thyroid carcinoma xenografts and suppresses tumor growth in nude mice. ERRγ-IN-1 is applicable for the research of anaplastic thyroid carcinoma .
|
-
- HY-105636
-
|
ICI 33828; Methallibure
|
Drug Derivative
GnRH Receptor
|
Endocrinology
|
|
Methallibure (ICI 33828) is a dithiocarbamoylhydrazine derivative and gonadotropic function blocker. Methallibure can block the action of pituitary gonadotropins in teleost fishes and inhibit germ cell maturation. Methallibure does not affect the histological structure of the thyroid gland but reduces the nuclear volume of thyroid epithelial cells. Methallibure can be used in the research of endocrine diseases .
|
-
- HY-N16764
-
|
|
Necroptosis
NO Synthase
|
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
(rel)-Salcolin A is a flavonoid lignan compound with anticancer, anti-inflammatory, and neuroprotective activities. (rel)-Salcolin A has IC50 values ??of 66.69 μM and 56.12 μM against anaplastic thyroid carcinoma cells (HTH83) and papillary thyroid carcinoma cells (TPC1), respectively. (rel)-Salcolin A also inhibits LPS-induced NO production with an IC50 of 14.65 μM. (rel)-Salcolin A exerts its effects by inducing necroptosis in thyroid cancer cells, inhibiting the production of the inflammatory factor NO, and protecting against glutamate-induced neuronal cell damage, with a neuroprotective E50 of 47.44 μM. (rel)-Salcolin A can be used in research related to thyroid cancer, anti-inflammation, and neuroprotection. (rel)-Salcolin A can be naturally extracted from the leaves of Casearia arborea and the stems of Zea mays (corn) .
|
-
- HY-159074
-
|
|
MAP3K
|
Inflammation/Immunology
Cancer
|
|
Cot-IN-5 (compound 1) is a potent ATP-competitive inhibitor of cancer osaka thyroid (COT). Cot-IN-5 can block COT kinase autophosphorylation .
|
-
- HY-183729
-
|
|
Ligands for Target Protein for PROTAC
RET
|
Endocrinology
Cancer
|
|
RET-IN-34 is a RET inhibitor with an IC50 of 0.89 nM. RET-IN-34 serves as a target protein ligand for PROTAC synthesis (Ligand for Target Protein for PROTAC). RET-IN-34 is applicable for the synthesis of PROTAC RET Degrader 2 (HY-183783). RET-IN-34 exhibits anticancer activity against medullary thyroid carcinoma. RET-IN-34 can be used in studies related to medullary thyroid carcinoma .
|
-
- HY-W008452R
-
-
- HY-183783
-
|
|
PROTACs
RET
STAT
ERK
Apoptosis
|
Endocrinology
Cancer
|
|
PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma .
|
-
- HY-178726
-
|
|
MAP3K
ERK
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
Cot-IN-4 (compound 32) is a potent cancer osaka thyroid (COT) kinase inhibitor with an IC50 of 6 nM. Cot-IN-4 inhibits the phosphorylation of ERK (IC50: 60 nM) and inhibits TNFα release (IC50: 60 nM). Cot-IN-4 also inhibits the formation of the pro-inflammatory cytokine IL-1β (IC50: 0.2 μM) in Uric acid (HY-B2130)-stimulated macrophages. Cot-IN-4 can be used for the study of inflammatory diseases .
|
-
- HY-183684
-
|
|
RET
VEGFR
PDGFR
Akt
ERK
|
Endocrinology
Cancer
|
|
RET-IN-33 is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer .
|
-
- HY-181555
-
|
|
Ras
|
Endocrinology
Cancer
|
|
IACS-56676 is a selective NRAS G12D inhibitor with a target IC50 of 0.031 μM. IACS-56676 stabilizes the p-loop, maintains key interactions with Asp12, Gly60 and Asp69, and achieves selectivity against wild-type KRAS through substitution targeting Leu95. IACS-56676 can be used in the research of melanoma, hematologic malignancies and thyroid cancer .
|
-
- HY-182741
-
|
|
RET
|
Endocrinology
Cancer
|
|
RET-IN-32 is an orally active RET inhibitor with IC50 values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer .
|
-
- HY-182485
-
|
|
Dopamine β-hydroxylase
|
Others
|
|
U-11634 is an orally active dopamine β-hydroxylase noncompetitive inhibitor, with rat LD50 values of 1197 mg/kg (subcutaneous) and 524 mg/kg (oral). U-11634 blocks conversion of dopamine to norepinephrine and reduces norepinephrine levels in brain. U-11634 decreases food intake and spontaneous motor activity via dietary inclusion. U-11634 induces thyroid toxicity and inhibits pregnancy. U-11634 inhibits deciduomata formation in intact and steroid-treated rats, with no reversal by progesterone or oestradiol. U-11634 can be used for pregnancy .
|
-
- HY-18957C
-
|
BGB-283 hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
|
-
- HY-107615R
-
|
|
Reference Standards
LPL Receptor
|
Cancer
|
|
TC LPA5 4 (Standard) is the analytical standard of TC LPA5 4 (HY-107615). This product is intended for research and analytical applications. TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened agent targets . TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells .
|
-
| Cat. No. |
Nombre del producto |
|
-
-
HY-L126
-
|
|
1,050 compounds
|
|
Nuclear receptors (NR) are proteins found in cells that sense androgen and thyroid hormones and certain other molecules. They are ligand-activated transcription factors that participate in many aspects of human physiology and pathology, and regulate the expression of various important genes.
Nuclear receptors have become one of the main targets in the development of new drug strategies, providing a unique type of receptors for studying a variety of human diseases, such as breast cancers, skin disorders and diabetes. 13% of U.S. Food and Drug Administration (FDA) approved drugs target nuclear receptors.
MCE supplies a unique collection of 1,050 nuclear receptor inhibitors and activators, all of which have the identified inhibitory or activated effect on nuclear receptor. MCE Nuclear Receptor Library is a useful tool for drugs research related to cancer, skin disease and diabetes.
|
| Cat. No. |
Nombre del producto |
Target |
Research Area |
-
- HY-W011258
-
|
L-Tyrosyl-L-phenylalanine
|
Xanthine Oxidase
Angiotensin-converting Enzyme (ACE)
|
Inflammation/Immunology
Cancer
|
|
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells .
|
| Cat. No. |
Nombre del producto |
Target |
Research Area |
Image |
-
- HY-P99165
-
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IGF-1R
TSH Receptor
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Endocrinology
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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 .
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(5)
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- HY-P99160
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hMN14
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Transmembrane Glycoprotein
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Cancer
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Labetuzumab is a humanised anti-carcinoembryonic antigen (CEA) monoclonal antibody that inhibits tumour growth and sensitises human medullary thyroid cancer xenografts to Dacarbazine chemotherapy .
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(5)
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- HY-P99364
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Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1
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VEGFR
Apoptosis
p38 MAPK
Akt
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Endocrinology
Cancer
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Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is an IgG1 antibody inhibitor targeting VEGFR-1/FLT1 with anti-tumor activity. By blocking ligand-dependent phosphorylation and downstream signal transduction, Icrucumab reduces the activities of MAPK and Akt in breast cancer xenograft models, inhibits the proliferation and invasion of VEGFR-1-positive tumor cells, and reverses the conversion of M1 macrophages to the pro-tumor M2-like phenotype. Icrucumab also inhibits tumor cell proliferation, promotes apoptosis, and effectively suppresses tumor growth through direct targeting of tumors and host support mechanisms. In addition, Icrucumab exhibits a synergistic effect when combined with chemotherapeutic agents, and it is used in research related to various cancers including advanced solid malignancies, thyroid cancer, melanoma, and lung cancer .
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(5)
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- HY-P991487
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Interleukin Related
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Inflammation/Immunology
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LASN01 is a human IgG1 monoclonal antibody (mAb) targeting IL-11RA. LASN01 inhibits IGF-1 and IL-11-induced hyaluronic acid (HA) release and TGFβ-stimulated procollagen in orbital fibroblasts. LASN01 can be used in thyroid eye disease (TED) research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
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(5)
| Cat. No. |
Nombre del producto |
Category |
Target |
Chemical Structure |
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- HY-13653
-
-
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- HY-N6033
-
|
(+)-Ferruginol
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Cupressaceae
Terpenoids
Diterpenoids
Thuja standishii (Gord.) Carr.
Plants
|
EBV
HSV
Apoptosis
|
|
Ferruginol ((+)-Ferruginol), a natural diterpenoid, is an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). Ferruginol inhibits the growth of thyroid cancer cells through the induction of mitochondrial apoptosis. Ferruginol has antitumor, cardioprotective, antioxidant, gastroprotective, and neuroprotective activities .
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-
- HY-B1234
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-
-
- HY-W017113
-
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|
Structural Classification
Productos naturales
Classification of Application Fields
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Source Classification
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Environmental Pollutants
Endogenous Metabolite
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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 .
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-
- HY-N0526
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|
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Flavonols
Structural Classification
Classification of Application Fields
Plants
Flavonoids
Pyrola calliantha H. Andr.
Pyrolaceae
Phenols
Polyphenols
Pyrola incarnata Fisch. ex DC.
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Sirtuin
Keap1-Nrf2
NF-κB
ERK
p38 MAPK
JNK
TSH Receptor
Reactive Oxygen Species (ROS)
SOD
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|
2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease .
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-
- HY-N0647
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-
-
- HY-W008452
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-
-
- HY-13653R
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-
-
- HY-114557
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|
3,5-Diiodo-L-thyronine
|
Structural Classification
Monophenols
Classification of Application Fields
Ketones, Aldehydes, Acids
Phenols
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Source Classification
|
JNK
NF-κB
Sirtuin
PGC-1α
COX
TGF-β Receptor
Collagen
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NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity .
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-
- HY-A0152
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-
-
- HY-N10348
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-
-
- HY-150526
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-
-
- HY-N6841
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-
-
- HY-N0885
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-
-
- HY-N0224A
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-
-
- HY-N0647R
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-
-
- HY-A0152R
-
-
-
- HY-114557R
-
|
3,5-Diiodo-L-thyronine (Standard)
|
Structural Classification
Monophenols
Ketones, Aldehydes, Acids
Phenols
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
|
|
NSC 90469 (Standard) is the analytical standard of NSC 90469. This product is intended for research and analytical applications. NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity .
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-
-
- HY-N0526R
-
|
|
Flavonols
Structural Classification
Flavonoids
Pyrola calliantha H. Andr.
Pyrolaceae
Phenols
Polyphenols
Plants
Pyrola incarnata Fisch. ex DC.
Source Classification
|
Reference Standards
Sirtuin
Keap1-Nrf2
NF-κB
ERK
p38 MAPK
JNK
TSH Receptor
Reactive Oxygen Species (ROS)
SOD
|
|
2"-O-Galloylhyperin (Standard) is the analytical standard of 2"-O-Galloylhyperin (HY-N0526). This product is intended for research and analytical applications. 2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease .
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-
-
- HY-N16764
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|
|
Structural Classification
Flavonoids
Flavones
Asteraceae
Phenols
Taraxacum officinale F. H. Wigg.
Plants
Source Classification
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Necroptosis
NO Synthase
|
|
(rel)-Salcolin A is a flavonoid lignan compound with anticancer, anti-inflammatory, and neuroprotective activities. (rel)-Salcolin A has IC50 values ??of 66.69 μM and 56.12 μM against anaplastic thyroid carcinoma cells (HTH83) and papillary thyroid carcinoma cells (TPC1), respectively. (rel)-Salcolin A also inhibits LPS-induced NO production with an IC50 of 14.65 μM. (rel)-Salcolin A exerts its effects by inducing necroptosis in thyroid cancer cells, inhibiting the production of the inflammatory factor NO, and protecting against glutamate-induced neuronal cell damage, with a neuroprotective E50 of 47.44 μM. (rel)-Salcolin A can be used in research related to thyroid cancer, anti-inflammation, and neuroprotection. (rel)-Salcolin A can be naturally extracted from the leaves of Casearia arborea and the stems of Zea mays (corn) .
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-
-
- HY-W008452R
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-
| Cat. No. |
Nombre del producto |
Chemical Structure |
-
- HY-13653S1
-
|
|
|
(-)-Epigallocatechin Gallate-d4 (EGCG-d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
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-
- HY-170017S
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(-)-Epigallocatechin Gallate-d3/d4 (EGCG-d3/d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
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-
-
- HY-B1234S
-
|
|
|
Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
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-
-
- HY-12753AS
-
|
|
|
Debutyldronedarone-d7 hydrochloride is deuterated labeled Debutyldronedarone hydrochloride (HY-12753A). Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
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-
-
- HY-W008452S
-
|
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H-Tyr(3-I)-OH- 13C6 is the 13C-labeled H-Tyr(3-I)-OH. H-Tyr(3-I)-OH is a potent and effective tyrosine hydroxylase inhibitor. H-Tyr(3-I)-OH is an intermediate in the production of thyroid hormones and has a role as a human or mouse metabolite .
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-
-
- HY-W713284
-
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2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
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