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SynKinase
(R)-BI-2536
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | (R)-BI2536 |
| Product Type | Chemical |
| Properties | |
| Formula | C28H39N7O3 |
| MW | 521.7 |
| CAS | 755038-02-9 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO, Ethanol |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: Plk1 | Kinase Group: Other | Substrate: Serine-Threonine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | XQVVPGYIWAGRNI-JOCHJYFZSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
Polo-like kinase 1 (Plk1) is a regulator of the cell cycle that has been implicated in the pathology of many cancers. BI-2536 is a potent and selective small-molecule inhibitor of mammalian Plk1. It has inhibitory activity at subnanomolar concentrations and inhibits tumor growth in multiple tumor lines with IC(50) values below 1µM. BI-2536 also shows an >1,000-fold selectivity for PIK1 versus a large panel of other kinases. BI-2536 also demonstrated low Kd values against sister kinases PLK2 and PLK3. Preclinical studies in human cancer cell lines have shown that BI 2536 disrupts spindle assembly, resulting in mitotic arrest and inducing apoptosis. BI-2536 is currently in clinical trials against several types of solid tumor cancers.
Product References
- BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo: M. Steegmaier, et al.; Curr. Biol. 17, 316 (2007)
- Pharmacophore modeling and virtual screening for designing potential PLK1 inhibitors: H.Y. Wang, et al.; Bioorg. Med. Chem. Lett. 18, 4972 (2008)
- Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors: Q. Zhang, et al.; Bioorg. Med. Chem. Lett. 22, 7615 (2012)
- HDAC inhibitors increase NRF2-signaling in tumour cells and blunt the efficacy of co-adminstered cytotoxic agents: M. McMahon, et al.; PLoS One 9, e114055 (2014)
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