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PARP1/BRD4-IN-2

PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) [1].

Product Specifications

CAS Number

3037993-97-5

UNSPSC

12352005

Target

Apoptosis; 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-2.html

Solubility

10 mM in DMSO

Smiles

O=C1C2=CC=CC=C2C(CC3=CC=CC(C4=NC5=CC(OC)=CC(OC)=C5C(N4)=O)=C3)=NN1

Molecular Formula

C25H20N4O4

Molecular Weight

440.45

References & Citations

[1]Zhang J, et al. Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy. J Med Chem. 2022 May 12;65 (9) :6803-6825.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

BRD4; PARP1

Frequently Asked Questions

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