BI 2536 | Dual Plk/BRD4 inhibitor – Destabilizes Myc
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $75.00 | ||
| 25 mg | $275.00 |
BI 2536 (755038-02-9) was originally reported as a potent (IC50’s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM)1 and selective2 Polo-like kinase inhibitor that caused mitotic arrest and apoptosis induction in various human cancer cell lines.1 It was later found to be a potent inhibitor (IC50 = 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells.3 BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1.4
References/Citations:
1) Steegmaier et al. (2007), BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo; Curr. Biol., 17 316
2) Davis et al. (2011), Comprehensive analysis of kinase inhibitor selectivity; Nat. Biotechnol., 29 1046
3) Ciceri et al. (2014), Dual kinase-bromodomain inhibitors for rationally designed polypharmacology; Nat. Chem. Biol., 10 305
4) Xiao et al. (2016), Polo-like Kinase-1 Regulates Myc Stabilization and Activates a Feedforward Circuit Promoting Tumor Cell Survival; Mol. Cell, 64 493
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
BI 2536 (755038-02-9) was originally reported as a potent (IC50’s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM)1 and selective2 Polo-like kinase inhibitor that caused mitotic arrest and apoptosis induction in various human cancer cell lines.1 It was later found to be a potent inhibitor (IC50 = 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells.3 BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1.4
References/Citations:
1) Steegmaier et al. (2007), BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo; Curr. Biol., 17 316
2) Davis et al. (2011), Comprehensive analysis of kinase inhibitor selectivity; Nat. Biotechnol., 29 1046
3) Ciceri et al. (2014), Dual kinase-bromodomain inhibitors for rationally designed polypharmacology; Nat. Chem. Biol., 10 305
4) Xiao et al. (2016), Polo-like Kinase-1 Regulates Myc Stabilization and Activates a Feedforward Circuit Promoting Tumor Cell Survival; Mol. Cell, 64 493
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