Name: CRT0044876
Price: 180.00 USD

- Overview
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    Background
    
    CRT0044876 is a potent and selective inhibitor of APE1 with IC50 value of 3.06 μM [1].
    Apurinic/apyrimidinic endonuclease-1 (APE1) is a member of the highly conserved exonuclease
    III family of AP endonucleases and plays an important role in DNA repair. APE1 exhibits 3’-phosphodiesterase activity and weak 3’-phosphatase activity, 3’-5’-exonuclease activity and RNaseH activity [1].
    CRT0044876 is a potent and selective APE1 inhibitor. In HeLa whole cell extract, CRT0044876 inhibited apurinic/apyrimidinic (AP) site cleavage catalyzed by APE1. CRT0044876 inhibited both the AP endonuclease and exonuclease activities of exonuclease III, the bacterial homologue of APE1. CRT0044876 inhibited the 3’-phosphoglycolate diesterase activity of APE1 with IC50 value of 5 μM and also inhibited 3’-phosphatase activity through binding to DNA repair active site of APE1. In HT1080 fibrosarcoma cells, CRT0044876 significantly increased AP site accumulation and was non-toxic at concentrations up to 400 μM. Also, CRT0044876 potentiated the cytotoxicity induced by alkylating agent MMS, temozolomide, hydrogen peroxide and hmdUrd through specific inhibition of the base excision repair (BER) pathway [1].
- Properties
  - Alternative Name
    
    7-nitro-1H-indole-2-carboxylic acid
    
    CAS Number
    
    6960-45-8
    
    Molecular Formula
    
    C9H6N2O4
    
    Molecular Weight
    
    206.15
    
    Appearance
    
    A solid
    
    Purity
    
    98.04%
    
    Solubility
    
    ≥55.56 mg/mL in DMSO; insoluble in H2O; ≥58.6 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CRT0044876

CRT0044876

Background

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