DY131 | GSK-9089 | CAS#95167-41-2 | ERRβ and ERRγ

DY131
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406664

CAS#: 95167-41-2

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.

Chemical Structure

DY131

CAS# 95167-41-2

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406664
Name: DY131
CAS#: 95167-41-2
Chemical Formula: C18H21N3O2
Exact Mass: 311.16
Molecular Weight: 311.385
Elemental Analysis: C, 69.43; H, 6.80; N, 13.49; O, 10.28

Price and Availability

Size	Price	Availability
100mg	USD 650	2 weeks
200mg	USD 950	2 weeks
500mg	USD 1450	2 weeks
1g	USD 2250	2 weeks
2g	USD 3650	2 weeks
5g	USD 5450	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist.
In vitro activity:	A selective ERRγ agonist, DY131, inhibited the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells. Reference: Int J Gynecol Cancer. 2012 Nov;22(9):1509-16. https://pubmed.ncbi.nlm.nih.gov/23051957/
In vivo activity:	Mice were pretreated with DY131 through intraperitoneal injection at a dose of 5 mg/kg/day for 3 days prior to LPS challenge (10 mg/kg). Pretreatment with DY131 ameliorated LPS-induced liver injury as demonstrated by reduced liver enzyme release (ALT, AST, and LDH), improved liver morphological damage, and attenuated oxidative stress, inflammation and apoptosis. Reference: Front Pharmacol. 2021 Apr 23;12:626166. https://pubmed.ncbi.nlm.nih.gov/33967760/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	2.0	6.42
	DMSO	36.5	117.33
	DMSO:PBS (pH 7.2) (1:1)	0.5	1.61
	Ethanol	3.1	10.00

Preparing Stock Solutions

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

Formulation protocol:	1. 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. PMID: 23051957. 2. 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. PMID: 22554036; PMCID: PMC3905677. 3. Ma H, Liu J, Du Y, Zhang S, Cao W, Jia Z, Gong W, Zhang A. Estrogen-Related Receptor γ Agonist DY131 Ameliorates Lipopolysaccharide-Induced Acute Liver Injury. Front Pharmacol. 2021 Apr 23;12:626166. doi: 10.3389/fphar.2021.626166. PMID: 33967760; PMCID: PMC8104008. 4. Huang B, Mu P, Yu Y, Zhu W, Jiang T, Deng R, Feng G, Wen J, Zhu X, Deng Y. Inhibition of EZH2 and activation of ERRγ synergistically suppresses gastric cancer by inhibiting FOXM1 signaling pathway. Gastric Cancer. 2021 Jan;24(1):72-84. doi: 10.1007/s10120-020-01097-x. Epub 2020 Jun 11. PMID: 32529327.
In vitro protocol:	1. 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. PMID: 23051957. 2. 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. PMID: 22554036; PMCID: PMC3905677.
In vivo protocol:	1. Ma H, Liu J, Du Y, Zhang S, Cao W, Jia Z, Gong W, Zhang A. Estrogen-Related Receptor γ Agonist DY131 Ameliorates Lipopolysaccharide-Induced Acute Liver Injury. Front Pharmacol. 2021 Apr 23;12:626166. doi: 10.3389/fphar.2021.626166. PMID: 33967760; PMCID: PMC8104008. 2. Huang B, Mu P, Yu Y, Zhu W, Jiang T, Deng R, Feng G, Wen J, Zhu X, Deng Y. Inhibition of EZH2 and activation of ERRγ synergistically suppresses gastric cancer by inhibiting FOXM1 signaling pathway. Gastric Cancer. 2021 Jan;24(1):72-84. doi: 10.1007/s10120-020-01097-x. Epub 2020 Jun 11. PMID: 32529327.

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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.

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