Search Result
Results for "
Thyroid Inhibitors
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-W010696
-
3′,5′,3-Triiodothyronine
|
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
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 .
|
-
-
- HY-B1234
-
Octyl methoxycinnamate
|
Androgen Receptor
Estrogen Receptor/ERR
Thyroid Hormone Receptor
Cytochrome P450
|
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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-
-
- HY-B1201
-
3,3',5-Triiodothyroacetic acid
|
Flavivirus
Thyroid Hormone Receptor
TNF Receptor
|
Endocrinology
|
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-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-122041
-
|
Apoptosis
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
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 .
|
-
-
- HY-W415287
-
-
-
- HY-N0224A
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(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 .
|
-
-
- 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 .
|
-
-
- HY-W010696R
-
|
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 .
|
-
-
- 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 .
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-
-
- HY-P99160
-
|
Transmembrane Glycoprotein
|
Cancer
|
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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-
-
- HY-141513
-
NH-3
3 Publications Verification
|
Thyroid Hormone Receptor
|
Neurological Disease
|
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-B1201R
-
|
Flavivirus
Thyroid Hormone Receptor
TNF Receptor
|
Endocrinology
|
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. .
|
-
-
- HY-115686
-
|
Adenosine Deaminase
|
Inflammation/Immunology
Cancer
|
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-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-14815
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Combretastatin A4 phosphate
|
Apoptosis
Microtubule/Tubulin
|
Cancer
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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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-
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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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-
-
- HY-19980A
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PRIMA-1
2 Publications Verification
NSC-281668
|
Autophagy
MDM-2/p53
Ferroptosis
Apoptosis
|
Cancer
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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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- 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-W011258
-
L-Tyrosyl-L-phenylalanine
|
Xanthine Oxidase
Angiotensin-converting Enzyme (ACE)
|
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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-
-
- HY-N0647
-
|
Monocarboxylate Transporter
|
Endocrinology
|
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 .
|
-
-
- 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-A0152
-
D-T4
|
Endogenous Metabolite
|
Metabolic Disease
|
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-N6033
-
(+)-Ferruginol
|
EBV
HSV
Apoptosis
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
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-W008452
-
|
Endogenous Metabolite
|
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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-
-
- HY-101246
-
|
RET
|
Cancer
|
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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-
-
- 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 .
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-
-
- HY-12753A
-
SR35021 hydrochloride
|
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
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-156113
-
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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-139915
-
|
Glutathione Peroxidase
|
Inflammation/Immunology
|
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-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 .
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-
-
- HY-N0647R
-
|
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-Y0470
-
Aminourea hydrochloride; Hydrazinecarboxamide hydrochloride
|
Monoamine Oxidase
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
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-Q04764
-
|
Thyroid Hormone Receptor
Apoptosis
|
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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-
-
- HY-153213
-
|
TSH Receptor
|
Metabolic Disease
|
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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-
-
- HY-A0152R
-
|
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 .
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-
-
- HY-156135
-
|
RET
|
Others
|
NSC194598 is a p53 DNA-binding inhibitor with IC50 value of 180 nM and 2-40 μM for in vitro and in vivo, respectively. NSC194598 interferes with transcriptional activation of mutated RET gene in human medullary thyroid carcinoma TT cells. NSC194598 can be used for acute toxicity to normal tissues by radiation and chemotherapy research .
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-
-
- 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 .
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-
-
- HY-12753AR
-
SR35021 (hydrochloride) (Standard)
|
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 .
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-
-
- HY-W017113
-
|
Endogenous Metabolite
Aryl Hydrocarbon Receptor
|
Metabolic Disease
|
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
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-
-
- HY-Y0470R
-
|
Antibiotic
|
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-13653
-
EGCG; Epigallocatechol Gallate
|
Endogenous Metabolite
Apoptosis
|
Inflammation/Immunology
Cancer
|
(-)-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 .
|
-
-
- HY-W009776
-
Suberohydroxamic acid; SBHA
|
HDAC
Apoptosis
|
Cancer
|
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) .
|
-
-
- HY-119459
-
|
Succinate Dehydrogenase
Fungal
Parasite
Constitutive Androstane Receptor
Caspase
NF-κB
|
Infection
Cancer
|
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-W008452S
-
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
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[1][2].
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-
-
- HY-132846
-
TAS0953/HM06
|
RET
Apoptosis
|
Cancer
|
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-107615
-
|
LPL Receptor
|
Cancer
|
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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-
-
- 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 .
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-
-
- HY-150526
-
|
Endogenous Metabolite
Apoptosis
|
Inflammation/Immunology
Cancer
|
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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-
-
- HY-145581
-
AZD4831
|
Glutathione Peroxidase
Cytochrome P450
|
Cardiovascular Disease
Inflammation/Immunology
|
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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-
- HY-13653R
-
EGCG(Standard); Epigallocatechol Gallate (Standard)
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Endogenous Metabolite
Apoptosis
|
Inflammation/Immunology
Cancer
|
(-)-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-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) .
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-
- HY-34596
-
|
Biochemical Assay Reagents
Amyloid-β
|
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 .
|
-
- HY-P99165
-
|
IGF-1R
TSH Receptor
|
Endocrinology
|
Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research .
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-
- HY-124828
-
|
HuR
|
Cancer
|
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-120026
-
KB015
|
Thyroid Hormone Receptor
|
Neurological Disease
|
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 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 opens large-conductance Ca 2+-activated K + channels and relaxes vascular smooth muscle .
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-
- HY-119459R
-
|
Succinate Dehydrogenase
Fungal
Parasite
Constitutive Androstane Receptor
Caspase
NF-κB
|
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-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-18957C
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BGB-283 hydrochloride
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Endogenous Metabolite
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Cancer
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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 .
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- HY-125535
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AMPK
mTOR
Autophagy
Atg8/LC3
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Cancer
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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-L126
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847 compounds
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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 847 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.
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Product Name |
Target |
Research Area |
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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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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99160
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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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- 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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Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B1234S
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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
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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[1][2].
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- HY-13653S1
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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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