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Description: Agonist selective for estrogen-related receptors ERRβ and ERRγ
Chemical Name: N-(4-(Diethylaminobenzylidenyl)-N'-(4-hydroxybenzoyl)-hydrazine
Purity: ≥99% (HPLC)
Biological Activity for DY131
DY131 is a selective agonist at estrogen-related receptors ERRβ (EC50 range = 130 - 698 nM in vitro) and ERRγ. Displays minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM. In a mouse model of hepatotoxicity, DY131 protects against LPS induced liver injury. Suppresses growth and proliferation of prostate, esophagus, gastric and breast cancer cells; concentration-dependently increases cell proliferation in T98G and U87MG cells (EC50 values are 54 nM and 62 nM respectively).
Compound Libraries for DY131
DY131 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for DY131
| M. Wt | 311.38 |
| Formula | C18H21N3O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 95167-41-2 |
| PubChem ID | 5497124 |
| InChI Key | WLKOCYWYAWBGKY-CPNJWEJPSA-N |
| Smiles | CCN(CC)C1=CC=C(C=C1)\C=N\NC(=O)C1=CC=C(O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for DY131
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 3.11 | 10 | |
| DMSO | 31.14 | 100 |
Preparing Stock Solutions for DY131
The following data is based on the product molecular weight 311.38. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.21 mL | 16.06 mL | 32.12 mL |
| 5 mM | 0.64 mL | 3.21 mL | 6.42 mL |
| 10 mM | 0.32 mL | 1.61 mL | 3.21 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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Product Datasheets for DY131
References for DY131
References are publications that support the biological activity of the product.
Yu and Forman (2005) Identification of an agonist ligand for estrogen-related receptors ERRβ/γ. Bioorg.Med.Chem.Lett. 15 1311 PMID: 15713377
Thouennon et al (2019) Insights into the activation mechanism of human estrogen-related receptor γ by environmental endocrine disruptors. Cell Mol.Life Sci. 76 4769 PMID: 31127318
Gandhari et al (2010) Identification and characterization of estrogen receptor-related receptor alpha and gamma in human glioma and astrocytoma cells. Mol.Cell Endocrinol. 315 314 PMID: 19822186
Heckler et al (2016) Antimitotic activity of DY131 and the estrogen-related receptor beta 2 (ERRβ2) splice variant in breast cancer. Oncotarget. 7 47201 PMID: 27363015
Zuercher et al (2005) Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma. J.Med.Chem. 48 3107 PMID: 15857113
Ma et al (2021) Estrogen-related receptor γ agonist DY131 ameliorates lipopolysaccharide-induced acute liver injury. Front.Pharmacol. 12 626166 PMID: 33967760
Wang et al (2023) ESRRG-PKM2 axis reprograms metabolism to suppress esophageal squamous carcinoma progression and enhance anti-PD-1 therapy efficacy. J.Transl.Med. 21 605 PMID: 37679788
If you know of a relevant reference for DY131, please let us know.
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Keywords: DY131, DY131 supplier, agonists, selective, estrogen-related, receptors, ERRβ, ERRbeta, ERRγ, ERRgamma, Estrogen, Receptors, ERRg, ERRb, and, Related, 2266, Tocris Bioscience
11 Citations for DY131
Citations are publications that use Tocris products. Selected citations for DY131 include:
Huang (2018) DA D1 Receptors Contribute Critically to the Apomorphine-Induced Inhibition of Form-Deprivation Myopia in Mice. Invest Ophthalmol Vis Sci 59 2623 PMID: 29847669
Tanida et al (2020) Novel metabolic system for lactic acid via LRPGC1/ERRγ signaling pathway FASEB J. 34 13239 PMID: 32851675
Heckler et al (2016) Antimitotic activity of DY131 and the estrogen-related receptor beta 2 (ERRβ2) splice variant in breast cancer. Oncotarget 7 47201 PMID: 27363015
Lu et al (2015) Messenger RNA profile analysis deciphers new Esrrb responsive genes in prostate cancer cells. Neuropharmacology 16 21 PMID: 26627478
Heckler and Riggins (2014) ERRβ splice variants differentially regulate cell cycle progression. Cell Cycle 14 31 PMID: 25496115
Luo et al (2014) Estrogen-related receptor γ serves a role in blood pressure homeostasis during pregnancy. Mol Endocrinol 28 965 PMID: 24725083
Kang et al (2018) Estrogen-related receptor gamma functions as a tumor suppressor in gastric cancer. Nat Commun 9 1920 PMID: 29765046
Byerly et al (2013) Estrogen-related receptor β deletion modulates whole-body energy balance via estrogen-related receptor γ and attenuates neuropeptide Y gene expression. Eur J Neurosci 37 1033 PMID: 23360481
Byerly et al (2013) Estrogen-related receptor β deficiency alters body composition and response to restraint stress. BMC Physiol 13 10 PMID: 24053666
Poidatz et al (2015) Trophoblast syncytialisation necessitates mitochondrial function through estrogen-related receptor-γ activation. Mol.Hum.Reprod. 21 206 PMID: 25376642
Gandhari et al (2010) Identification and characterization of estrogen receptor-related receptor alpha and gamma in human glioma and astrocytoma cells. Mol Cell Endocrinol 315 314 PMID: 19822186
Do you know of a great paper that uses DY131 from Tocris? Please let us know.
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