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26744
BI 2536
Activators & Inhibitors
Chemical Modulators

BI 2536 #26744

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BI 2536: Image 1

Chemical structure of BI 2536.

Product Usage Information

BI 2536 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 958 μl of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 521.7 g/mol
Purity

>97%

Molecular Formula

C28H39N7O3

CAS 755038-02-9
Solubility Soluble in DMSO at 20 mg/ml or ethanol at 25 mg/ml.

Background

BI 2536 is a small molecule inhibitor of mammalian polo-like kinases (PLKs) with a strong selectivity for PLK1 (IC50 = 0.83 nM) (1). PLK1 is important in regulating mitosis and is often overexpressed in cancers, contributing to excessive cell proliferation and loss of key checkpoint functions (1,2). Research indicates that BI 2536 causes mitotic arrest and apoptosis in 32 unique human cancer cell lines and inhibits the growth of human tumor xenografts in nude mice, with little to no effect on healthy cells (1,3). This along with the fact that BI 2536 exhibits high permeability through the blood-brain barrier, makes it an important therapeutic tool (4). BI 2536 inhibits BRD4 (IC50 = 100 nM) and BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells (5). Recently, BRD4 inhibition has shown anti-viral activity and increased host resistance to several DNA and RNA viruses, making BRD4 disruptors important compounds to study in relation to viral diseases (6).

  1. Steegmaier, M. et al. (2007) Curr Biol 17, 316-22.
  2. Lee, S.Y. et al. (2014) Dev Reprod 18, 65-71.
  3. Liu, X. et al. (2006) Mol Cell Biol 26, 2093-108.
  4. Danovi, D. et al. (2013) PLoS One 8, e77053.
  5. Ciceri, P. et al. (2014) Nat Chem Biol 10, 305-12.
  6. Wang, J. et al. (2020) PLoS Pathog 16, e1008429.

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 # 26744S
Product # Size Price
26744S
5 mg $ 131