95167-41-2

95167-41-2 structure

Name: DY131
Chemical Name: DY131
CAS Number: 95167-41-2
Molecular Formula: C₁₈H₂₁N₃O₂
Molecular Weight: 311.378
Catalog: Research Areas Cancer
Create Date: 2017-03-27 14:35:49
Modify Date: 2024-01-07 18:19:49
DY131(GSK 9089) is a novel selective agonist of ERRβ and ERRγ; displays minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.IC50 value:Target: ERRβ/γDY131, a selective ERRγ agonist, could potentiate the ERRγ-induced growth inhibition in LNCaP- ERRγ and DU145- ERRγ cells in a dose-dependent manner compared with respective parental cells. DY131 inhibited the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells. DY131 had no effect on the structurally related receptors ERRα or the estrogen receptors alpha and beta (ERalpha/beta). DY131 appears to inhibit Smo signaling through a common binding site shared by previously reported Smo agonists and antagonists.

Name	DY131
Synonyms	Benzoic acid, 4-hydroxy-, 2-[(1E)-[4-(diethylamino)phenyl]methylene]hydrazide N'-{(E)-[4-(diethylamino)phenyl]methylidene}-4-hydroxybenzohydrazide N'-{(E)-[4-(Diethylamino)phenyl]methylene}-4-hydroxybenzohydrazide Benzoic acid, 4-hydroxy-, [[4-(diethylamino)phenyl]methylene]hydrazide (9CI) N-(4-(Diethylaminobenzylidenyl)-N'-(4-hydroxybenzoyl)-hydrazine GSK 9089

Description	DY131(GSK 9089) is a novel selective agonist of ERRβ and ERRγ; displays minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.IC50 value:Target: ERRβ/γDY131, a selective ERRγ agonist, could potentiate the ERRγ-induced growth inhibition in LNCaP- ERRγ and DU145- ERRγ cells in a dose-dependent manner compared with respective parental cells. DY131 inhibited the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells. DY131 had no effect on the structurally related receptors ERRα or the estrogen receptors alpha and beta (ERalpha/beta). DY131 appears to inhibit Smo signaling through a common binding site shared by previously reported Smo agonists and antagonists.
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
References	[1]. Wang Y, Arvanites AC, Davidow L,et al. Selective identification of hedgehog pathway antagonists by direct analysis of smoothened ciliary translocation . ACS Chem Biol. 2012,15;7(6):1040-8. [2]. Kumar P, Mendelson CR. Estrogen-related receptor gamma (ERRgamma) mediates oxygen-dependent induction of aromatase (CYP19) gene expression during human trophoblast differentiation. Mol Endocrinol. 2011;25(9):1513-26. [3]. Yamamoto T, Mori T, Sawada M, et al. Estrogen-related receptor-γ regulates estrogen receptor-α responsiveness in uterine endometrial cancer. Int J Gynecol Cancer. 2012;22(9):1509-16. [4]. Yu S, Wang X, Ng CF, et al. ERRgamma suppresses cell proliferation and tumor growth of androgen-sensitive and androgen-insensitive prostate cancer cells and its implication as a therapeutic target for prostate cancer. Cancer Res. 2007;67(10):4904-14. [5]. Donna D. Yu, Barry Marc Forman. Identification of an agonist ligand for estrogen-related receptors ERRβ/γ. Bioorganic & Medicinal Chemistry Letters. 2005,15(5): 1311-1313.

Density	1.1±0.1 g/cm3
Molecular Formula	C₁₈H₂₁N₃O₂
Molecular Weight	311.378
Exact Mass	311.163391
PSA	64.93000
LogP	3.17
Index of Refraction	1.574
Storage condition	2-8°C

Hazard Codes	Xi: Irritant;
Risk Phrases	36/37/38
Safety Phrases	26-36
HS Code	2928000090

5351-23-5

120-21-8

~66%

95167-41-2

Literature: Forman, Barry; Yu, Donna Patent: US2006/189825 A1, 2006 ; Location in patent: Page/Page column 7; 12; Sheet 3/7 ; US 20060189825 A1

3290-99-1

95167-41-2

Literature: Bioorganic and Medicinal Chemistry Letters, , vol. 15, # 5 p. 1311 - 1313

120-21-8

95167-41-2

Literature: Bioorganic and Medicinal Chemistry Letters, , vol. 15, # 5 p. 1311 - 1313

123-08-0

120-21-8

95167-41-2

Literature: Journal of Medicinal Chemistry, , vol. 48, # 9 p. 3107 - 3109

Precursor 4
5351-23-5 120-21-8 3290-99-1 123-08-0
DownStream 0

HS Code	2928000090
Summary	2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%