Ixazomib

SKU: orb1306436

Description

Ixazomib

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 1072833-77-2
• MW: 361.03
• Purity: 99.77%
• Formula: C₁₄H₁₉BCl₂N₂O₄
• SMILES: CC(C)C[C@H](NC(=O)CNC(=O)c1cc(Cl)ccc1Cl)B(O)O
• Target: Autophagy,Caspase,Proteasome
• Solubility: Ethanol:9 mg/mL (24.93 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.54 mM);DMSO:55 mg/mL (152.34 mM)

Bioactivity

• Target IC50:
  Caspase-like β1:3 nM|20S proteasome:0.93 nM(Ki)|20S proteasome:3.4 nM|Trypsin like β2:3500 nM
• In Vivo:
  MLN2238 is a biologically active metabolite of MLN9708.MLN2238 and Bortezomib are both time-dependent reversible inhibitors o the proteasome, bu the isolated half-life o the proteasomal effect of MLN2238 (18 min) is 6-fold faster compared with that of Bortezomib (110 min).The oncological efficacy of MLN2238 is higher than that of Bortezomib. MLN2238 is a nitrogen-terminally capped dipeptide leucine borate that inhibit the hydrolysis site of chymotrypsin-like enzymes in the 20S proteasome IC50 Ki: 3.4/0.93 nM). At higher concentration , MLN2238 also inhibite the caspase-like hydrolysis site IC50 31 nM) an the trypsin-like hydrolysis site IC50 3.5 μM) o the 20S proteasome.MLN2238 inhibited Calu-6 cells IC50 9.7 nM).
• In Vitro:
  MLN2238 is a biologically active metabolite of MLN9708.MLN2238 and Bortezomib are both time-dependent reversible inhibitors o the proteasome, bu the isolated half-life o the proteasomal effect of MLN2238 (18 min) is 6-fold faster compared with that of Bortezomib (110 min).The oncological efficacy of MLN2238 is higher than that of Bortezomib. MLN2238 is a nitrogen-terminally capped dipeptide leucine borate that inhibit the hydrolysis site of chymotrypsin-like enzymes in the 20S proteasome IC50 Ki: 3.4/0.93 nM). At higher concentration , MLN2238 also inhibite the caspase-like hydrolysis site IC50 31 nM) an the trypsin-like hydrolysis site IC50 3.5 μM) o the 20S proteasome.MLN2238 inhibited Calu-6 cells IC50 9.7 nM).
• 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: store at low temperature | 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, caspase-like (β1), Autophagy, Inhibitor, inhibit, Ixazomib, MLN 2238, MLN2238, MLN-2238, Proteasome

Compound Identifiers

PubChem CID

25183872