BI 2536|755038-02-9|BI-2536|BI2536|(R)-4-((8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide|UNII-4LJG22T9C6|4LJG22T9C6|4-{[(7r)-8-Cyclopentyl-7-Ethyl-5-Methyl-6-Oxo-5,6,7,8-Tetrahydr
Specifications & Purity
Moligand™, ≥98%
Biochemical and Physiological Mechanisms
BI 2536 treatment ranging from 10 nM to 100 nM blocks the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibits of cohesin release from chromosome arms, and induces monopolar spindle formation and other Plk1 dependent proce
Storage Temp
Protected from light,Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Serine/threonine-protein kinase PLK1 inhibitor
Product Description
BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM. It shows 4- and 11-fold greater selectivity against Plk2 and Plk3. A Plk inhibitor with efficacy against 32 cancer cell lines.
1.Steegmaier M, Hoffmann M, Baum A, Lénárt P, Petronczki M, Krssák M, Gürtler U, Garin-Chesa P, Lieb S, Quant J et al.. (2007) BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.. Curr Biol, 17 (4):(316-22). [PMID:17291758]
2.Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C et al.. (2014) Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.. Nat Chem Biol, 10 (4):(305-12). [PMID:24584101]
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B1615031