GeA-69

Research use only, not for human use.

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

GeA-69 (compound 1) (50 μM and 250 μM; pre-damage for 1 h or 0.5, 1, 2.5 min) engages PARP14 MD2 in intact cells and prevents its localisation to sites of DNA damage in U-2 OS cells. GeA-69 (25 nM-250 μM; 72 h) exhibits moderate cytotoxicity among HeLa, U-2 OS and HEK293 cells and highly cell permeable with 2 % passing paracellular and 98 % transcellular over the membrane. Cell Cytotoxicity Assay Cell Line:HeLa, U-2 OS and HEK293 cells Concentration:25 nM-250 μM Incubation Time:72 hours Result:Resulted moderate cytotoxicity against normal cells with EC50_HeLa=58 μM, EC50_U-2 OS=52 μM, EC50_HEK293=54 μM.

——

——

Cell Cycle/DNA Damage

PARP

PARP14

——

——

2143475-98-1

300.36

C20H16N2O

>98% (HPLC)

DMSO: 120 mg/mL (399.53 mM)

CC(=O)Nc1ccccc1-c1cccc2c3ccccc3[nH]c12

N-(2-(9H-carbazol-1-yl)phenyl)acetamide

(-20℃)

With Ice Pack

≥ 2 years