Description
MLN2238 shows inhibition to 20S proteasome with IC50 of 3.4 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C14H19BCl2N2O4
Chemical Name
(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid
Solubility
DSMO 72 mg/mL Water
In vitro
MLN2238 is an N-capped dipeptidyl leucine boronic acid and it can inhibitthe chymotrypsin-like proteolytic (beta5) site of the 20S proteasome with an IC 50 value of 3.4 nmol/L and Ki of 0.93 nM. MLN2238 is similar to MLN9708. Actually, MLN2238 is the biologically active form of MLN9708, and MLN9708 immediately hydrolyzed to MLN2238 on exposure to aqueous solutions or plasma. As a potent inhibitor of the proteasome, MLN2238 lead to stabilization and accumulation of ubiquitinated proteins, resulting in cell cycle disruption, activation of apoptotic pathways, and active cell death.
In vivo
MLN2238 shows antitumor activity in the CWR22 xenograft model MLN2238 dosed at 14 mg/kg twice weekly and showed similar antitumor activity (T/C = 0.36) with bortezomib dosed at 0.8 mg/kg twice weekly . In WSU-DLCL2 xenograft model, MLN2238 dosed at 14 mg/kg twice weekly showed strong antitumor activity (T/C = 0.36), however, bortezomib dosed at 0.8 mg/kg twice weekly can not potently inhibit tumors.(T/C=0.79)
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