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Ixazomib

Catalog No. T2122 CAS 1072833-77-2

Synonyms: MLN 2238, MLN-2238, Ixazomib, Inhibitor, MLN2238, inhibit, Proteasome, Autophagy

MLN2238, a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM).

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Ixazomib, CAS 1072833-77-2

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Purity: 98%

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Storage & Solubility Information

Description	MLN2238, a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM).
Targets&IC50	caspase-like (β1):31nM, 20S proteasome:0.93 nM(Ki), 20S proteasome:3.4 nM, trypsin-like (β2):3500 nM
Kinase Assay	Kinase assay : Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents according to the manufacturer's instructions. Luminescence is measured using a LEADseeker instrument.
Cell Research	Calu-6 cells are cultured in MEM containing 10% FBS and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentrations of Bortezomib or MLN2238 in DMSO (0.5% final, v/v) for 1 hour at 37 °C. For reversibility experiments, cells are treated with either 1 μM Bortezomib or MLN2238 for 30 minutes at 37 °C and then washed thrice in medium to remove the Bortezomib or MLN2238. Cells are incubated for an additional 4 hours at 37 °C, after which the medium is removed and replaced with fresh medium. (Only for Reference)

Synonyms	MLN 2238, MLN-2238, Ixazomib, Inhibitor, MLN2238, inhibit, Proteasome, Autophagy
Molecular Weight	361.03
Formula	C14H19BCl2N2O4
CAS No.	1072833-77-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 67 mg/mL (185.6 mM)

Ethanol: 9 mg/mL (24.92 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature

1. Kupperman E, et al. Cancer Res, 2010, 70(5), 1970-80 1. Chen X, Chen Y, Ou Y, et al. Bortezomib inhibits NLRP3 inflammasome activation and NF-κB pathway to reduce psoriatic inflammation. Biochemical Pharmacology. 2022, 206: 115326. 2. Lee EC, et al. Clin Cancer Res, 2011, 17(23), 7313-23.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Autophagy Compound Library HIF-1 Signaling Pathway Compound Library Inhibitor Library Drug-induced Liver Injury (DILI) Compound Library Immunology/Inflammation Compound Library Covalent Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library

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