PARP-1/2-IN-2

PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively) . PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor[1].

Product Specifications

CAS Number

[3052304-23-8]

UNSPSC

12352005

Target

Apoptosis; CDK; PARP

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/parp-1-2-in-2.html

Solubility

10 mM in DMSO

Smiles

NC(C1=CC=CC2=C1N=C(NC(C3=CC(C(N4CCC(NC5=NC=C(I)C=N5)CC4)=O)=CC=C3)=O)N2)=O

Molecular Formula

C25H23IN8O3

Molecular Weight

610.41

References & Citations

[1]Zhang L, et al. Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer. Eur J Med Chem. 2023 Jul 16;259:115648.