BI 2536

BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively[1]. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription[4].

Product Specifications

CAS Number

[755038-02-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Epigenetic Reader Domain; Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bi-2536.html

Purity

99.95

Solubility

0.1 M HCl : 25 mg/mL (ultrasonic; adjust pH to 4 with HCl) |DMSO : 65 mg/mL (ultrasonic)

Smiles

O=C1[C@H](N(C2=C(N1C)C=NC(NC3=CC=C(C(NC4CCN(C)CC4)=O)C=C3OC)=N2)C5CCCC5)CC

Molecular Formula

C28H39N7O3

Molecular Weight

521.65

Precautions

H302, H315, H319, H335

References & Citations

[1]Lénárt P, et al. The Small-Molecule Inhibitor BI 2536 Reveals Novel Insights into Mitotic Roles of Polo-like Kinase 1. Curr Biol. 2007 Feb 20;17 (4) :304-15.|[2]Chen L, et al. BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett. 2015 May 18;6 (7) :764-9.|[3]Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Current Biology (2007), 17 (4), 316-322.|[4]Malik N, et al. Suppression of IFN β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15;468 (3) :363-72.