DY-131

SKU: orb1222970

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.

Key Properties

• CAS Number: 95167-41-2
• MW: 311.38
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₁N₃O₂
• SMILES: C(=O)(c1ccc(cc1)O)N/N=C/c1ccc(cc1)N(CC)CC
• Target: Ephrin Receptor
• Solubility: DMSO : 50 mg/mL. 160.58 mM

Bioactivity

• 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. Animal model: Mature male mice (C57BL/6) (8-10 week-old; ~24.3 g). Dosage: 5 μg/kg. Administration: Subcutaneous injection; every second day; for 12 days. Result: Increased P450scc, StAR and HMGCR while decreased HSL expressions.
• 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. DY131 inhibits 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. DY131 dramatically decreases phosphorylated histone H3 (pH3) marked proliferation of CGNPs induced by Shh. A selective ERRγ agonist, DY131, inhibits the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells. Cell Proliferation Assay 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DY131 | DY-131 | DY 131 | GSK-9089

Quick Database Links

Gene Symbol

Ephrin Receptor