BRD4/CK2-IN-1

BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC) [1]

Product Specifications

CAS Number

[2756851-99-5]

UNSPSC

12352005

Target

Apoptosis; Autophagy; Casein Kinase; Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Cell Cycle/DNA Damage; Epigenetics; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/brd4-ck2-in-1.html

Purity

98.21

Solubility

DMSO : 20 mg/mL (ultrasonic; warming; adjust pH to 3 with HCl; heat to 60°C)

Smiles

O=C1C2=C(OC)C=C(OC)C=C2N=C(C3=CC=C(OCC(NC4=CC(Cl)=C(N5CCN(C)CC5)C=C4)=O)C=C3)N1

Molecular Formula

C29H30ClN5O5

Molecular Weight

564.03

References & Citations

[1] Zhang J, et al. Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy. J Med Chem. 2021;64 (24) :18025-18053.