GeA-69

GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a Kd value of 2.1 μM. GeA-69 involves in DNA damage repair mechanisms and prevents recruitment of PARP14 MD2 to sites of laser-induced DNA damage[1][2].

Product Specifications

CAS Number

[2143475-98-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

PARP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gea-69.html

Purity

99.91

Solubility

DMSO : ≥ 125 mg/mL

Smiles

CC(NC1=CC=CC=C1C2=CC=CC3=C2NC4=C3C=CC=C4)=O

Molecular Formula

C20H16N2O

Molecular Weight

300.35

Precautions

H302, H315, H319, H335

References & Citations

[1]Schuller M, et al. Discovery of a Selective Allosteric Inhibitor Targeting Macrodomain 2 of Polyadenosine-Diphosphate-Ribose Polymerase 14. ACS Chem Biol. 2017 Nov 17;12 (11) :2866-2874.|[2]Moustakim M, et al. Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2. Bioorg Med Chem. 2018 Jul 15;26 (11) :2965-2972.