Brief Description

MLN4924 is a potent and selective small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50 = 4.7 nM).
IC50 value: 4.7 nM
Target: NAE
At much higher concentrations, MLN 4924 inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 values of 1.5 and 8.2 μM, respectively. At 0.3 μM, MLN 4924 has been shown to disrupt CRL-mediated protein turnover leading to apoptosis in HCT-116 cells by deregulating S-phase DNA synthesis. In vivo, 30-60 mg/kg MLN 4924 dose-dependently suppresses the growth of human tumor xenografts in mice.

Solubility

DMSO > 50 mg/ml

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light yellow to yellow solid