CRT0044876 (Synonyms: CRT0044876, 7-Nitroindole-2-Carboxylic Acid, NSC 69877) |
Catalog No.GC17231 |
CRT0044876은 강력하고 선택적인 아퓨린/아피리미딘 엔도뉴클레아제 1(APE1) 억제제(IC50=~3μM)입니다. CRT0044876은 APE1의 AP 엔도뉴클레아제, 3'-포스포디에스테라아제 및 3'-포스파타아제 활성을 억제하며, APE1이 속하는 효소의 엑소뉴클레아제 III 계열의 특정 억제제입니다. CRT0044876은 여러 DNA 염기 표적 화합물의 세포독성을 강화합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 6960-45-8
Sample solution is provided at 25 µL, 10mM.
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].
Reference:
[1]. Madhusudan S, Smart F, Shrimpton P, et al. Isolation of a small molecule inhibitor of DNA base excision repair. Nucleic Acids Res, 2005, 33(15): 4711-4724.
Average Rating: 5
(Based on Reviews and 33 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *