Description
MLN9708 can inhibit CT-L Proteasome and 20S proteasome with IC50 of 5 nM and 3.4 nM.
Storage
2 years at -20centigrade Powder
Targets
CT-L Proteasome, 20S proteasome
Molecular Formula
C20H23BCl2N2O9
Chemical Name
4-(carboxymethyl)-2-((R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dioxaborinane-4-carboxylic acid
Solubility
DMSO 103 mg/mL Water
In vitro
MLN9708, a selective, orally bioavailable, second-generation proteasome inhibitor. MLN2238 is the biologically active form of MLN9708. In studies where a solution of MLN9708 was added directly into rat, dog, or human plasma and immediately extracted and analyzed by HPLC, only MLN2238 could be identified. At higher concentrations, it also inhibited the caspase-like ( beta 1) and trypsin-like ( beta 2) proteolytic sites (IC 50 of 31 and 3,500 nmol/L).
In vivo
MLN2238 inhibits growth of xenografted human MM cells in CB-17 SCID mice.
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