SMER3

SKU: orb1940369

Description

SMER 3 is an inhibitor of the Skp1-Cullin-F-box (SCF)(Met30) ubiquitin ligase, a member of the SCF E3-ligase family, which regulates diverse cellular processes including transcription, cell-cycle control and immune response.(In Vitro):SMER 3 and rapidly increased PFKFB3 protein levels. Accordingly, ubiquitin-bound PFKFB3 was lower in E2- or G1-treated HUVECs. Both agents increased deubiquitinase USP19 levels through GPER signaling.(In Vivo):SMER 3 diminishes binding of the F-box subunit Met30 to the SCF core complex in vivo and show evidence for SMER 3 directly binding to Met30.

Key Properties

• CAS Number: 67200-34-4
• MW: 224.18
• Purity: >98% (HPLC)
• Formula: C₁₁H₄N₄O₂
• SMILES: O=C1C2=CC=CC=C2C3=NC4=NON=C4N=C31
• Target: mGluR5
• Solubility: In Vitro: DMSO : 12.5 mg/mL (55.76 mM)

Bioactivity

• In Vitro:
  In yeast cells, Met4 ubiquitination is blocked in cells exposed to SMER3 (0-60 μM). The met4Δ cells are less susceptible to growth inhibition by SMER3.Addition of SMER3 to the ligase reactions inhibited ubiquitination of Met4 by SCFMet30 in a dose-dependent manner. SMER3 significantly inhibits the binding of Met30 to Skp1, and does not affect the Skp1 and Met30 protein levels.

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

SMER 3 | SMER3

Quick Database Links

Gene Symbol

mGluR5