XMD17-109

SKU: orb1226284

Description

XMD17-109 is a novel, specific ERK-5 inhibitor with an EC50 4.2 uM in HEK293 cells.

Key Properties

• CAS Number: 1435488-37-1
• MW: 638.81
• Purity: >98% (HPLC)
• Formula: C₃₆H₄₆N₈O₃
• SMILES: CN1CCN(C2CCN(C(C3=CC(OCC)=C(NC4=NC=C5C(N(C6CCCC6)C(C=CC=C7)=C7C(N5C)=O)=N4)C=C3)=O)CC2)CC1
• Target: ERK
• Solubility: Ethanol: 100 mg/mL (156.54 mM); DMSO: 100 mg/mL (156.54 mM)

Bioactivity

• In Vitro:
  XMD17-109 (Compound 26) inhibits ERK5 biochemically with an IC50 of 0.162 ± 0.006 μM, and blocks pidermal growth factor induced ERK5 autophosphorylation with an EC50 of 0.09 ± 0.03 μM in cells. XMD17-109 also inhibits LRRK2[G2019S] with an IC50 of 339 nM. XMD17-109 demonstrats low nanomolar cellular activity judged by the significant dose-dependent reduction of mobility shifted phosphorylated ERK5 bands from sorbitol stimulated cells. XMD17-109 completely inhibits the ERK5-mediated AP1 transcriptional activity at 30 μM and has an EC50 of 4.2 μM.

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

ERK5-IN-1

Quick Database Links

Gene Symbol

ERK