BI 2536
BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy.
Inquire / Order:
manager@chemfaces.com
Technical Inquiries:
service@chemfaces.com
Tel:
+86-27-84237783
Fax:
+86-27-84254680
Address:
1 Building, No. 83, CheCheng Rd., Wuhan Economic and Technological Development Zone, Wuhan, Hubei 430056, PRC
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
Green Chemistry2021, ISSUE 2.
J. Traditional Thai Medical Res. 2022,8(1):1-14.
ACS Omega.2024, 9(12):14356-14367.
Eur J Pharmacol.2023, 950:175772.
Evid Based Complement Alternat Med.2021, 8707280.
J Pharm Anal.2016, 6(6):363-373
Foods2023, 12(23), 4342.
Nat Prod Communications2018, 10.1177
Molecules.2024, 29(6):1392.
Foods.2023, 12(2):318.
Related and Featured Products
Cancer Res,2009 Mar 1;69(5):1916-23.
Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma.[Pubmed:
19223553]
Anaplastic thyroid carcinoma (ATC) is one of the most aggressive and chemoresistant cancers. The serine/threonine kinase Polo-like kinase 1 (PLK1), a key regulator of multiple steps during mitotic progression, is highly expressed in ATC.
METHODS AND RESULTS:
Here, we used the BI 2536 PLK1 inhibitor on ATC and nontransformed thyroid follicular cell lines. Our data show that ATC cells are addicted to high levels of PLK1 activity for proliferation, survival, anchorage-independent growth, and tumorigenicity. On treatment with nanomolar doses of BI 2536, ATC cells progressed normally through S phase but died thereafter, directly from mitotic arrest. Immunofluorescence microscopy, immunoblot, and flow cytometry analysis showed that, on PLK1 blockade, ATC cells arrested in prometaphase with a 4N DNA content. Treated ATC cells accumulated phosphohistone H3 and displayed characteristic mitotic (Polo) spindle aberrations. Nontransformed thyroid cells were 3.2- to 18.4-fold less susceptible to BI 2536-induced cell cycle effects compared with ATC cells.
CONCLUSIONS:
These findings identify PLK1 as a promising target for the molecular therapy of ATC.
Curr Biol,2007 Feb 20;17(4):316-22.
BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.[Pubmed:
17291758]
Cell lines: HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji and PC-3 cells, etc.
Concentrations: Dissolved in DMSO, final concentrations ~1 μM
Incubation Time: 24 and 72 hours
Method:
Cells are exposed to various concentrations of BI 2536 for 24, and 72 hours. Cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. For determining the DNA content of the cultures, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide (PI) in PBS for 20 minutes at RT. Cell-cycle profiles are determined by flow cytometric analysis.
