Cat. No. Name Size Price Add Cart
KI3112MLN-22385 mg$272
MLN-223810 mg$512
MLN-2238200 mg$3952

Chemical Characteristic

Product NameMLN-2238
CAS No.1072833-77-2
Molecular Weight 361.03
FormulaC14H19BCl2N2O4
Chemical Name[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]butanoyl]amino]-3-methylbutyl]boronic acid
Smiles[C@H](CC(C)C)(B(O)O)NC(=O)CNC(=O)c1c(ccc(c1)Cl)Cl
Chemical Structure

Biological activities

MLN2238 is a selective, potent, and reversible inhibitor of the proteasome. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM. Meanwhile, MLN2238 also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50s of 31 and 3500 nM, respectively. In vivo, MLN2238 shows antitumor activity in the CWR22 xenograft model, and induces a greater pharmacodynamic response than bortezomib in xenograft tumors.[1]

Protocols

In vivo, MLN2238 is dissolved in DMSO.[1]

References

[1]Kupperman E, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010, 70(5): 1970-1980.

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