| Identification | Back Directory | [Name]
4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE | [CAS]
101574-65-6 | [Synonyms]
CS-1084 4-hydroxy-N'-(4-isopropylbenzylidene)benzohydrazide (E)-4-hydroxy-N'-(4-isopropylbenzylidene)benzohydrazide 4-HYDROXY-2-[(1E)-[4-(1-METHYLETHYL)PHENYL]METHYLENE]HYDRAZIDE 2-[[4-(1-Methylethyl)phenyl]methylene]hydrazide 4-hydroxybenzoic acid 4-Hydroxybenzoic acid 2-[[4-(1-methylethyl)phenyl]methylene]hydrazide Benzoic acid, 4-hydroxy-, 2-[[4-(1-methylethyl)phenyl]methylene]hydrazide | [Molecular Formula]
C17H18N2O2 | [MDL Number]
MFCD00567155 | [MOL File]
101574-65-6.mol | [Molecular Weight]
282.34 |
| Chemical Properties | Back Directory | [density ]
1.12 | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO: >10mg/mL | [form ]
powder | [pka]
8.48±0.15(Predicted) | [color ]
white to off-white |
| Hazard Information | Back Directory | [Description]
The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the estrogen receptor family and are expressed in tissues with high metabolic demand. Binding of peroxisome proliferator-activated receptor γ-coactivator 1α (PGC-1α) to this class of receptors is known to potentiate ERR activity. GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand, PGC-1α. It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors. This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise. | [Uses]
The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the estrogen receptor family and are expressed in tissues with high metabolic demand. Binding of peroxisome proliferator-activated receptor γ-coactivator 1α (PGC-1α) to this class of receptors is known to potentiate ERR activity. GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand, PGC-1α. It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors. This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.[Cayman Chemical] | [Definition]
ChEBI:GSK 4716 is a monoterpenoid. | [Biological Activity]
Selective agonist at estrogen-related receptors ERR β and ERR γ . Displays selectivity over ERR α and the classical estrogen receptors. | [storage]
Store at -20°C | [References]
[1] LIPING WANG. X-ray crystal structures of the estrogen-related receptor-gamma ligand binding domain in three functional states reveal the molecular basis of small molecule regulation.[J]. The Journal of Biological Chemistry, 2006: 37773-37781. DOI: 10.1074/jbc.m608410200 [2] SHAMINA M RANGWALA. Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity.[J]. The Journal of Biological Chemistry, 2010, 285 29: 22619-22629. DOI: 10.1074/jbc.m110.125401 |
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