WNY0824

WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models[1][2].

Product Specifications

CAS Number

[2412707-81-2]

Product Name Alternative

PLK1/BRD4-IN-1

UNSPSC

12352005

Target

Androgen Receptor; Apoptosis; c-Myc; Epigenetic Reader Domain; Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Vitamin D Related/Nuclear Receptor

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/wny0824.html

Solubility

10 mM in DMSO

Smiles

O=C(NC1CCN(C)CC1)C2=CC=C(NC(N=C3N(CC4CCCCC4)[C@@H]5CC)=NC=C3N6C5=NN=C6C)C(OC)=C2

Molecular Formula

C31H43N9O2

Molecular Weight

573.73

References & Citations

[1]Ning-Yu Wang, et al. Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors. Eur J Med Chem. 2020 Apr 1;191:112152.|[2]Ying Xu, et al. "Novel dual BET and PLK1 inhibitor WNY0824 exerts potent antitumor effects in CRPC by inhibiting transcription factor function and inducing mitotic abnormality." Molecular Cancer Therapeutics 19.6 (2020) : 1221-1231.