PLK1/BRD4-IN-3

PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1) . PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC50s of 0.059, 0.127 and 0.245 μM, respectively[1].

Product Specifications

CAS Number

[2251709-91-6]

UNSPSC

12352005

Target

Epigenetic Reader Domain; Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/plk1-brd4-in-3.html

Purity

99.66

Solubility

DMSO : 16.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1[C@H](C)N(C2CCCC2)C3=NC(NC4=CC=C(C(NC5CCN(C)CC5)=O)C=C4OC6CCCC6)=NC=C3N1C

Molecular Formula

C31H43N7O3

Molecular Weight

561.72

References & Citations

[1]Liu S, et al., Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4) /Polo-like Kinase 1 (PLK1) Inhibitors. J Med Chem. 2018 Sep 13;61 (17) :7785-7795.