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Nuclear Receptor/Transcription Factor

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Cat. No. Product Name Field of Application Chemical Structure
DC46879 (S)-Coriolic acid
(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury.
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DC46878 AMG131
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM).
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DC45607 JNJ-63576253 (TRC-253) Featured
JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.
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DC46688 Sevelamer-(d5)n hydrochloride
Sevelamer-(d5)n hydrochloride is the deuterium labeled Sevelamer hydrochloride. Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
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DC46556 Super-TDU (1-31)
Super-TDU (1-31) is a peptide of Super-TDU, which is an inhibitor of YAP-TEADs, shows potent anti-tumor activity.
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DC46525 Super-TDU TFA
Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model.
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DC46490 GNE-502
GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer.
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DC46381 SBC-115337
SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM.
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DC46311 TAT-cyclo-CLLFVY TFA
TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
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DC46307 Norgestimate D6
Norgestimate D6 is the deuterium labeled Norgestimate. Norgestimate, a synthetic progesterone analog, is an orally active progestin with highly selective progestational activity and minimal androgenicity. Norgestimate is used for an oral contraceptive.
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DC46235 Keap1-Nrf2-IN-1 TFA
Keap1-Nrf2-IN-1 TFA (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 TFA activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models.
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DC46177 AHR antagonist 5 hemimaleate
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).
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DC46033 Miroestrol
Miroestrol is a highly active phytoestrogen. Miroestrol can produce mammogenic effect. Miroestrol exhibits bone loss prevention and neuroprotective in ovariectomized mice. Miroestrol also can reduce cancer risk.
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DC45979 GNE-274
GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research.
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DC45910 AKB-6899
AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects.
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DC45909 AHR antagonist 5 free base
AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases.
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DC45908 6,2',4'-Trimethoxyflavone
6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction.
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DC45884 Honokiol DCA
Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level.
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DC45882 Dehydrocurdione
Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase (HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity.
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DC45837 MYC-IN-2
MYC-IN-2 is a MYC protein-protein inhibitor. MYC-IN-2 can be used for the research of cancer.
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DC45793 TRC160334
TRC160334 is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 can be used for the research of ischemia/reperfusion injury.
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DC45775 Arzoxifene
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile.
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DC45609 NH-3
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.
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DC45608 FK614
FK614 is an orally active, potent, selective PPARγ modulator (SPPARM). FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 is a nonthiazolidinedione insulin sensitizer. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.
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DC45606 CLP-3094
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
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DC45484 16α-Hydroxytrametenolic acid
16α-Hydroxytrametenolic acid, a natural triterpene, is a potential retinoid X receptor (RXR) selective agonist.
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DC45379 Tibolone
Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
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DC45378 GPR30 agonist-1
GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1 exerts vasorelaxant effects.
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DC45355 1α-Hydroxy-3-epi-vitamin D3
1α-Hydroxy-3-epi-vitamin D3, a natural metabolite of 1alpha,25-dihydroxyvitamin D3, is a potent suppressor of parathyroid hormone (PTH) secretion.
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DC45348 NY2267
NY2267 is a disruptor of Myc-Max interaction, with an IC50 of 36.5 μM.
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