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MedKoo Cat#: 406664 | Name: DY131
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Description:

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

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
DY131
CAS#95167-41-2

Theoretical Analysis

MedKoo Cat#: 406664

Name: DY131

CAS#: 95167-41-2

Chemical Formula: C18H21N3O2

Exact Mass: 311.1634

Molecular Weight: 311.39

Elemental Analysis: C, 69.43; H, 6.80; N, 13.49; O, 10.28

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 4,250.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Related CAS #
No Data
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
View handling instruction
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/
Solvent mg/mL 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
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

Recalculate based on batch purity %
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.
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, Dieudonné 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.