PARP1 PROTAC 180055

PARP1 PROTAC 180055 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively) . PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A) ; Blue: E3 ligase VHL ligand (HY-125845) ; Black: linker (HY-W014787) ) [1].

Product Specifications

UNSPSC

12352005

Target

PARP; PROTACs

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C1NCCC2=C(C3=CC=C(CN(C)C(CCCCCCCCC(N[C@H](C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)C(C)(C)C)=O)=O)C=C3)NC7=CC(F)=CC1=C72

Molecular Formula

C51H62FN7O6S

Molecular Weight

920.14

References & Citations

[1]Chen L, et al. Minimizing DNA trapping while maintaining activity inhibition via selective PARP1 degrader. Cell Death Dis. 2024 Dec 18;15 (12) :898.