Product Details
| Product Name:
Marizomib |
CAS No.:
437742-34-2 |
| Purity:
98.03% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | Marizomib |
| Description | Marizomib is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM.[3] |
| In vitro | METHODS: TNBC (basal), ductal and non-malignant breast epithelial cells were treated with Marizomib (0-500 nM) and cell proliferation was analyzed using the MTS assay after 6 days.
RESULTS Marizomib selectively reduced TNBC cell proliferation in a concentration-dependent manner without much effect on non-TNBC and non-malignant mammary epithelial cells (MCF10A and D492), with IC50 values of Marizomib less than 150 nM in TNBC cell lines and greater than 1 μM in non-TNBC cell lines.[1]
METHODS: SUM159PT cells were treated with 100 nM Marizomib for 0 and 9 hours (prior to induction of apoptosis) and label-free global proteomics analysis was performed to identify proteins or pathways altered by Marizomib.
RESULTS A total of 2547 proteins were identified, of which 425 proteins were downregulated (log2 ≤ 0.6) and 293 proteins were upregulated (log2 ≥ 0.6).Marizomib decreased the levels of 11 proteasome subunits, and 5 proteasome subunits (PSMA5, PSMC2, PSMD2, PSMA1, PSMA7 and PSMA8) were also observed to be Up-regulation. [1]
METHODS: Cells were treated with 40 nM or 80 nM marizomib for 4 h. CT-L activity of proteasome in total cell lysates was determined by lysing Suc-LLVY-AMC.
RESULTS marizomib effectively inhibited proteasomes in both responsive and non-responsive cells. [2] |
| In vivo | METHODS: After two weeks of Marizomib (0.15 mg/kg twice/week, IP) treatment of MDA-MB-231 xenografts and patient-derived tumor xenografts (PDX), it was observed whether tumor growth was inhibited in vivo.
RESULTS Marizomib treatment significantly reduced tumor volume and tumor weight in MDA-MB-231 xenografts and patient-derived tumor xenografts (PDX). [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 31.38 mg/mL (100 mM)
|
| Keywords | NPI 0052 | Marizomib | ML-858 | NPI0052 | ML 858 |
| Inhibitors Related | Sitagliptin | Sitagliptin phosphate monohydrate | Vildagliptin | 4'-Hydroxychalcone |
| Related Compound Libraries | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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$2.00/1KG |
VIP6Y
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Career Henan Chemical Co
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2020-01-08 |
United States