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BI 2536 | Dual Plk/BRD4 inhibitor - Destabilizes Myc

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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Catalog#  10-4121-0005

$75.00
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CAS:
755038-02-9
Catalog Number:
10-4121
Activity:
Dual Plk/BRD4 inhibitor - Destabilizes Myc
Chemical Name:
4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Molecular Weight:
521.67
Molecular Formula:
C28H39N7O3
Solubility:
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
97% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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