CDK4/6/BRD4-IN-2

CDK4/6/BRD4-IN-2 (Compound PJ2) is a dual inhibitor of CDK4/6 and BRD4 with IC50 values for CDK4, CDK6, BRD4 (BD1), and BRD4 (BD2) of 168.75, 292.45, 23.17, and 3.12 nM respectively. CDK4/6/BRD4-IN-2 has a strong inhibitory effect on non-small cell lung cancer (NSCLC) cell lines. CDK4/6/BRD4-IN-2 induces cell cycle arrest, senescence and apoptosis through ROS-mediated DNA damage. CDK4/6/BRD4-IN-2 can also effectively inhibit the migration and invasion of NCI-H358 cells. CDK4/6-IN-2 can be used for the study of KRAS-mutated NSCLC[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; CDK; Discoidin Domain Receptor; DNA/RNA Synthesis; Reactive Oxygen Species (ROS)

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

CC(C1=CN=C(NC2=CC=C(N3CCN(CCNC(C[C@H]4C5=NN=C(C)N5C(SC(C)=C6C)=C6C(C7=CC=C(Cl)C=C7)=N4)=O)CC3)C=N2)N=C1N8C9CCCC9)=C(C(C)=O)C8=O

Molecular Formula

C45H49ClN12O3S

Molecular Weight

873.47

References & Citations

[1]Tong X, et al. Design, synthesis, and biological evaluation of novel CDK4/6 and BRD4 dual inhibitors for treatment of KRAS-mutant NSCLC. Eur J Med Chem. 2025 Aug 5;292:117685.