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15022
Carfilzomib
Activators & Inhibitors
Chemical Modulators

Carfilzomib #15022

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Carfilzomib: Image 1

Chemical structure of carfilzomib.

Carfilzomib: Image 2

Western blot analysis of extracts from NIH/3T3 cells, untreated (-) or treated with Carfilzomib (6 hr) at the indicated concentrations, using Ubiquitin Antibody #3933.

Carfilzomib: Image 3

Western blot analysis of extracts from NIH/3T3 cells, untreated (-) or treated with Carfilzomib (6 hr) at the indicated concentrations, using p53 (1C12) Mouse mAb #2524 (upper) or β-Actin (13E5) Rabbit mAb #4970 (lower).

Product Usage Information

Carfilzomib is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 1 mg of powder in 277.82 μl of DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 20-2000 nM for 4-48 hours.

Storage

Store lyophilized or in solution at -20ºC, desiccated. The chemical is stable for 24 months in lyophilized form. Once in solution, use within 1 week to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 719.9 g/mol
Purity

>98%

Molecular Formula

C40H57N5O7

CAS 868540-17-4
Solubility Soluble in DMSO at 80mg/ml and EtOH at 25mg/ml.

Background

Carfilzomib, also known as PR-171, is a potent and irreversible epoxomycin-related proteasome inhibitor (1-4). It preferentially inhibits the chymotrypsin-like (CT-L) activity (low nanomolar IC50) of the 20S proteasome with greater than ten-fold selectivity over trypsin-like and caspase-like activities (1,2). CT-L inhibition with carfilzomib prevents degradation of short-lived misfolded and ubiquitinated proteins intended for proteasomal degradation, inducing cell cycle arrest and/or apoptosis in a variety of tumor cell lines (1-3). Carfilzomib has been shown to have greater antiproliferative activity against multiple myeloma (MM) cells than bortezomib and can overcome bortezomib-induced drug resistance (1). Synergistic interactions between carfilzomib and the histone deacetylase inhibitors vorinostat and entinostat have been observed (4). Proteasome inhibitors such as carfilzomib are important research tools for studying cellular degradation of the ubiquitin-proteasome pathway.

This product has applications to SARS-CoV-2 research into the mechanisms of the Novel Coronavirus, which has caused the COVID-19 pandemic.

  1. Kuhn, D.J. et al. (2007) Blood 110, 3281-90.
  2. Demo, S.D. et al. (2007) Cancer Res 67, 6383-91.
  3. Sacco, A. et al. (2011) Clin Cancer Res 17, 1753-64.
  4. Dasmahapatra, G. et al. (2011) Mol Cancer Ther 10, 1686-97.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST's products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST's Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
To Purchase # 15022S
Product # Size Price
15022S
1 mg $ 75