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GeA-69

CAS No. 2143475-98-1

GeA-69( —— )

Catalog No. M20135 CAS No. 2143475-98-1

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GeA-69
  • Note
    Research use only, not for human use.
  • Brief Description
    GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).
  • Description
    GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).
  • 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.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP14
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2143475-98-1
  • Formula Weight
    300.36
  • Molecular Formula
    C20H16N2O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 120 mg/mL (399.53 mM)
  • SMILES
    CC(=O)Nc1ccccc1-c1cccc2c3ccccc3[nH]c12
  • Chemical Name
    N-(2-(9H-carbazol-1-yl)phenyl)acetamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.
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