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  3. DY131

DY131 (Synonyms: GSK 9089)

Cat. No.: HY-15483 Purity: 99.72%
Handling Instructions

DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ. DY131 also inhibits Smo signaling.

For research use only. We do not sell to patients.

DY131 Chemical Structure

DY131 Chemical Structure

CAS No. : 95167-41-2

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10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
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Description

DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ[1][2]. DY131 also inhibits Smo signaling[3].

IC50 & Target[2]

ERRγ

 

ERRβ

 

In Vitro

DY131 (0.1-30 μM; 5 days) treatment suppresses cell proliferation and reduces BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner, with higher suppression in LNCaP-ERRγ clone[1].
DY131inhibits Shh induced accumulation of Smo::EGFP with an IC50 of 0.8 μM. DY131 suppresses SAG (100 nM) induced accumulation of Smo::EGFP in the primary cilium and Gli transcription activity with an IC50 of ~2 μM[3].
DY131 dramatically decreases phosphorylated histone H3 (pH3) marked proliferation of CGNPs induced by Shh[3].
A selective ERRγ agonist, DY131, inhibits the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: LNCaP-ERRγ and LNCaP cells
Concentration: 0.1 μM, 1 μM, 10 μM, 30 μM
Incubation Time: 5 days
Result: Suppressed cell proliferation and reduced BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner.
In Vivo

DY131 (5 μg/kg; subcutaneous injection; every second day; for 12 days) treatment increases P450 side-chain cleavage (P450scc), StAR and HMGCoA reductase (HMGCR) while decreases hormone sensitive lipase (HSL) expressions[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mature male mice (C57BL/6) (8-10 week-old; ~24.3 g)[5]
Dosage: 5 μg/kg
Administration: Subcutaneous injection; every second day; for 12 days
Result: Increased P450scc, StAR and HMGCR while decreased HSL expressions.
Molecular Weight

311.38

Formula

C₁₈H₂₁N₃O₂

CAS No.

95167-41-2

SMILES

O=C(N/N=C/C1=CC=C(N(CC)CC)C=C1)C2=CC=C(O)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (160.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2115 mL 16.0576 mL 32.1151 mL
5 mM 0.6423 mL 3.2115 mL 6.4230 mL
10 mM 0.3212 mL 1.6058 mL 3.2115 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.03 mM); Suspended solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DY131GSK 9089DY 131DY-131GSK9089GSK-9089Estrogen Receptor/ERRSmoSmoothenedERRβERRγP450sccStARHMGCRHSLInhibitorinhibitorinhibit

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