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MLN2238 is an inhibitor of the ?5 subunit of the 20S proteasome (IC50 = 3.4 nM in a cell-free assay) and an active metabolite of MLN9708 (Item No. 18386).{31628,31627} It is formed from MLN9708 via hydrolysis in plasma.{31628} MLN2238 is selective for the chymotrypsin-like ?5 subunit over the caspase-like ?1 and trypsin-like ?2 subunits (IC50s = 31 and 3,500 nM, respectively). It also binds caseinolytic protease P (Kd = 5,700 nM) and prevents hemolysis of isolated ovine erythrocytes induced by methicillin-resistant S. aureus (MRSA; EC50 = 3,600 nM).{58924} MLN2238 inhibits the proliferation of A375 and H460 lung and HCT116 and HT-29 colon cancer cells (IC50s = 20, 58, 19, and 52 nM, respectively) as well as osteoclastogenesis in peripheral blood mononuclear cells (PBMCs) isolated from patients with multiple myeloma (IC50 = 4.8 nM).{31628,31627} It reduces tumor growth in a CWR22 prostate cancer mouse xenograft model when administered at a dose of 14 mg/kg. Formulations containing MLN2238 have been used in the treatment of multiple myeloma.
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 5 mg, 50 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1072833-77-2 |
| Molecular formula | C14H19BCl2N2O4 |
| Smiles | ClC1=C(C(NCC(N[C@H](B(O)O)CC(C)C)=O)=O)C=C(Cl)C=C1 |
| Molecular weight | 361 |
| Custom code | 2922.19 |
| Formulation | A crystalline solid |
| Purity | ≥95% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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