PARP1/BRD4-IN-3

PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; DNA/RNA Synthesis; Epigenetic Reader Domain; PARP

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/parp1-brd4-in-3.html

Smiles

O=S(C1=CC=C(F)C(C)=C1)(NC2=CC3=C(NC(C(CC)=C3)=O)C=C2)=O

Molecular Formula

C18H17FN2O3S

Molecular Weight

360.40

References & Citations

[1]Feng B, et al. Combining Data-Driven and Structure-Based Approaches in Designing Dual PARP1-BRD4 Inhibitors for Breast Cancer Treatment. J Chem Inf Model. 2024 Oct 14;64 (19) :7725-7742.