PARP1/BRD4-IN-1

PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively) . PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells[1].

Product Specifications

CAS Number

[2758117-74-5]

UNSPSC

12352005

Target

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

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/parp1-brd4-in-1.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CC=CC2=C1NC(CN3C(N(C)C4=CC=C(C5=C(C)ON=C5C)C=C4C3C6=CC=CC=C6)=O)=N2)N

Molecular Formula

C29H26N6O3

Molecular Weight

506.56

References & Citations

[1]Huang SH, et al. Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer. Eur J Med Chem. 2022;230:114116.