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GeA-69

SKU: orb1221005

Description

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

Images & Validation

Key Properties

CAS Number2143475-98-1
MW300.36
Purity>98% (HPLC)
FormulaC20H16N2O
SMILESCC(=O)Nc1ccccc1-c1cccc2c3ccccc3[nH]c12
TargetPARP
SolubilityDMSO: 120 mg/mL (399.53 mM)

Bioactivity

In Vitro
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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GeA-69 (orb1221005)

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200 mg
500 mg
5 mg
$ 110.00
10 mg
$ 160.00
25 mg
$ 280.00
50 mg
$ 480.00
100 mg
$ 640.00