DMX-5804

SKU: orb1225584

Description

DMX-5804 (DMX5804) is a potent, selective small-molecule inhibitor of MAP4K4 with IC50 of 3 nM; displays >100-fold selectivity over GCK/MAP4K2, GLK/MAP4K3, KHS/MAP4K5 and VEGFR; rescues cell survival, mitochondrial function, and calcium cycling in hiPSC-CMs (human induced-pluripotent-stem-cell-derived cardiomyocytes), protects hiPSC-CMs with EC50 of 500 nM for cell death induced by 400 uM H2O2; reduces infarct size and ischemia-reperfusion injury in mice in mice.

Key Properties

• CAS Number: 2306178-56-1
• MW: 361.401
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₉N₃O₃
• SMILES: O=C1NC=NC2=C1C(C3=CC=C(OCCOC)C=C3)=CN2C4=CC=CC=C4
• Target: MAP4K
• Solubility: DMSO : 125 mg/mL 345.89 mM

Bioactivity

• In Vitro:
  DMX-5804 exhibits great selectivity at MAP4K4 over other kinases, such as GCK/MAP4K2 (pIC50, 6.50), GLK/MAP4K3 (pIC50, 4.95), KHS/MAP4K5 (pIC50, 6.36), ABL1 (pIC50, 5.80), Aurora B (pIC50, 5.49), FLT3 (pIC50, 5.31), GSK3β (pIC50, 4.66), MLK1/MAP3K9 (pIC50, 7.19), MLK3/MAP3K11 (pIC50, 6.99), NUAK (pIC50, 6.88) and VEGFR (pIC50, 5.72).
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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

DMX5804 | DMX 5804

Quick Database Links

Gene Symbol

MAP4K