WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406664
Description: DY131, also known as GSK-9089, is a novel selective agonist at estrogen-related receptors ERRβ and ERRγ. DY131 could potentiate the ERRgamma-induced growth inhibition in LNCaP-ERRgamma and DU145-ERRgamma cells in a dose-dependent manner. ERRgamma may perform an antiproliferative or tumor-suppressing function in prostate cancer cells. ERRgamma could be a novel therapeutic target for prostate cancer treatment.
MedKoo Cat#: 406664
Chemical Formula: C18H21N3O2
Exact Mass: 311.16338
Molecular Weight: 311.39
Elemental Analysis: C, 69.43; H, 6.80; N, 13.49; O, 10.28
Synonym: DY131; DY-131; DY 131; GSK-9089; GSK 9089; GSK9089.
IUPAC/Chemical Name: (E)-N'-(4-(diethylamino)benzylidene)-4-hydroxybenzohydrazide
InChi Key: WLKOCYWYAWBGKY-CPNJWEJPSA-N
InChi Code: InChI=1S/C18H21N3O2/c1-3-21(4-2)16-9-5-14(6-10-16)13-19-20-18(23)15-7-11-17(22)12-8-15/h5-13,22H,3-4H2,1-2H3,(H,20,23)/b19-13+
SMILES Code: CCN(C1=CC=C(/C=N/NC(C2=CC=C(O)C=C2)=O)C=C1)CC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 311.39 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||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Vanacker JM, Maiorano D. Checking the cycle by ERRβ splice variants. Cell Cycle. 2015 Mar 19:0. [Epub ahead of print] PubMed PMID: 25789879.
2: Heckler MM, Riggins RB. ERRβ splice variants differentially regulate cell cycle progression. Cell Cycle. 2015;14(1):31-45. doi: 10.4161/15384101.2014.972886. PubMed PMID: 25496115.
3: Poidatz D, Dos Santos E, Gronier H, Vialard F, Maury B, De Mazancourt P, DieudonnÃ© MN. Trophoblast syncytialisation necessitates mitochondrial function through estrogen-related receptor-γ activation. Mol Hum Reprod. 2015 Feb;21(2):206-16. doi: 10.1093/molehr/gau102. Epub 2014 Nov 6. PubMed PMID: 25376642.
4: Luo Y, Kumar P, Chen CC, Latham J, Wang L, Tudela C, Alexander JM, Shelton JM, McKown L, Mendelson CR. Estrogen-related receptor γ serves a role in blood pressure homeostasis during pregnancy. Mol Endocrinol. 2014 Jun;28(6):965-75. doi: 10.1210/me.2014-1003. Epub 2014 Apr 11. PubMed PMID: 24725083; PubMed Central PMCID: PMC4042076.
5: Byerly MS, Swanson RD, Wong GW, Blackshaw S. Estrogen-related receptor β deficiency alters body composition and response to restraint stress. BMC Physiol. 2013 Sep 22;13:10. doi: 10.1186/1472-6793-13-10. PubMed PMID: 24053666; PubMed Central PMCID: PMC3850731.
6: Yamamoto T, Mori T, Sawada M, Kuroboshi H, Tatsumi H, Yoshioka T, Matsushima H, Iwasaku K, Kitawaki J. Estrogen-related receptor-γ regulates estrogen receptor-α responsiveness in uterine endometrial cancer. Int J Gynecol Cancer. 2012 Nov;22(9):1509-16. doi: 10.1097/IGC.0b013e31826fd623. PubMed PMID: 23051957.
7: Wang Y, Arvanites AC, Davidow L, Blanchard J, Lam K, Yoo JW, Coy S, Rubin LL, McMahon AP. Selective identification of hedgehog pathway antagonists by direct analysis of smoothened ciliary translocation. ACS Chem Biol. 2012 Jun 15;7(6):1040-8. doi: 10.1021/cb300028a. Epub 2012 May 3. PubMed PMID: 22554036; PubMed Central PMCID: PMC3905677.
8: 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 Sep;25(9):1513-26. doi: 10.1210/me.2011-1012. Epub 2011 Jul 14. PubMed PMID: 21757507; PubMed Central PMCID: PMC3165917.
9: Yu S, Wong YC, Wang XH, Ling MT, Ng CF, Chen S, Chan FL. Orphan nuclear receptor estrogen-related receptor-beta suppresses in vitro and in vivo growth of prostate cancer cells via p21(WAF1/CIP1) induction and as a potential therapeutic target in prostate cancer. Oncogene. 2008 May 22;27(23):3313-28. Epub 2007 Dec 10. PubMed PMID: 18071305.
10: Yu S, Wang X, Ng CF, Chen S, Chan FL. 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 May 15;67(10):4904-14. PubMed PMID: 17510420.
11: Yu DD, Forman BM. Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1311-3. PubMed PMID: 15713377.