MLN9708

• CAT Number: I000957
• CAS Number: 1239908-20-3
• Molecular Formula: C20H23BCl2N2O9
• Molecular Weight: 517.12
• Purity: ≥95%
• Target: 20S Proteasome
• Solubility: DMSO 103 mg/mL; Water <1 mg/mL
• Storage: -20°C
• IC50: 3.4 nM (MLN2238)
• IUPAC Name: (R)-2,2'-(2-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-5-oxo-1,3,2-dioxaborolane-4,4-diyl)diacetic acid
• InChI: InChI=1S/C20H23BCl2N2O9/c1-10(2)5-14(21-33-19(32)20(34-21,7-16(27)28)8-17(29)30)25-15(26)9-24-18(31)12-6-11(22)3-4-13(12)23/h3-4,6,10,14H,5,7-9H2,1-2H3,(H,24,31)(H,25,26)(H,27,28)(H,29,30)/t14-/m0/s1
• InChIKey: MBOMYENWWXQSNW-AWEZNQCLSA-N
• SMILES: O=C(O)CC1(OB(OC1=O)C(NC(=O)CNC(=O)C2=CC(Cl)=CC=C2Cl)CC(C)C)CC(=O)O

MLN9708 (CAT: I000957), also known as ixazomib, is a proteasome inhibitor developed as an anticancer agent. It belongs to the class of boron-containing compounds and is a second-generation proteasome inhibitor derived from bortezomib. MLN9708 selectively and reversibly inhibits the chymotrypsin-like activity of the 20S proteasome, which plays a crucial role in protein degradation and cellular homeostasis. By inhibiting the proteasome, MLN9708 disrupts protein turnover, accumulating misfolded or unwanted proteins and subsequent induction of apoptosis in cancer cells. It has shown efficacy in various hematologic malignancies and solid tumors and has been approved for treating multiple myeloma.

Reference

[1]. Kupperman E, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010 Mar 1;70(5):1970-80.
[2]. Chauhan D, et al. In vitro and in vivo selective antitumor activity of a novel orally bioavailable proteasome inhibitor MLN9708 against multiple myeloma cells. Clin Cancer Res. 2011 Aug 15;17(16):5311-21.
[3]. Tian Z, et al. Investigational agent MLN9708/2238 targets tumor-suppressor miR33b in MM cells. Blood. 2012 Nov 8;120(19):3958-67.