MLN9708 analogues

SKU: orb1306735

Description

MLN2238, the biologically active form of Ixazomib (MLN9708), is a potent and selective inhibitor of the 20S proteasome's chymotrypsin-like (β5) activity (Ki50=0.93 nM, IC50=3.4 nM). This investigational small molecule is widely used in preclinical research, including in vitro cell-based assays and in vivo xenograft models, to study proteasome function and cancer therapeutics.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 1201902-80-8
• MW: 517.12
• Purity: 99.23%
• Formula: C₂₀H₂₃BCl₂N₂O₉
• SMILES: CC(C)C[C@H](NC(=O)CNC(=O)c1cc(Cl)ccc1Cl)B1OC(=O)CC(CC(O)=O)(O1)C(O)=O
• Target: Autophagy,Proteasome
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.38 mM);DMSO:93 mg/mL (179.84 mM)

Bioactivity

• Target IC50:
  20S proteasome:0.93 nM(Ki)|20S proteasome:3.4 nM
• In Vivo:
  Upon contact with aqueous solutions and plasma, MLN9708 rapidly hydrolyzes into MLN2238, which possesses bioactivity. MLN2238 inhibit the chymotrypsin-like hydrolytic sites o the 20S proteasome IC50 3.4 nM,K = .93 nM]). It also inhibit the caspase-like IC50 31 nM]) and trypsin-like hydrolytic sites IC50 3.5 μM]) o the 20S proteasome.
• In Vitro:
  MLN9708 exhibits anticancer activity in a variety of solid tumors and hematologic malignancies.
• Cell Research:
  Calu-6 cells are cultured in MEM containing 10% FBS and 1% penicillin/streptomycin and plated 1 day befor the start o the experiment at 1 × 104 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentration of Bortezomib or MLN2238 in DMSO (0.5% final, v/v) for 1 hour at 37℃. For reversibility experiments, cells are treated with either 1 μM Bortezomib or MLN2238 for 30 minutes at 37℃nd then washed thrice in medium to remov the Bortezomib or MLN2238. Cells are incubated for an additional 4 hours at 37℃, after whic the medium is removed and replaced with fresh medium. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

20S proteasome, MLN9708, MLN-9708, MLN 9708, Ixazomib Citrate analogues

Compound Identifiers

PubChem CID

49867936