PARP1/2/TNKS1/2-IN-1

PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, TNKS1 and TNKS2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis[1].

Product Specifications

CAS Number

[2243453-32-7]

UNSPSC

12352005

Target

Apoptosis; 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/parp1-2-tnks1-2-in-1.html

Solubility

10 mM in DMSO

Smiles

O=C(N1CCN(C(C2=CC(CC3=NNC(C4=C3C=CC=C4)=O)=CC=C2F)=O)CC1)NC5=CC=C(C(NC6=CC=C(OC)C=C6)=O)C=C5

Molecular Formula

C35H31FN6O5

Molecular Weight

634.66

References & Citations

[1]Xu Y, et al. Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy. Eur J Med Chem. 2022 Jul 5;237:114417.