规格: | 98% |
分子量: | 284.27 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Background:
FEN1-IN-3 (Compound 4) is a human flap endonuclease-1 (hFEN1) inhibitor. FEN1-IN-3 stabilizes hFEN1 with an EC50 of 6.8 μM[1].
FEN1 inhibition selectively impairs proliferation of colon cancer cells deficient in Cdc4 and Mre11a, both frequently mutated in colorectal cancers. FEN1 has also emerged as a potential chemosensitizing target due to its role in LP-BER since it is critical for repair of Methyl methanesulfonate-induced alkylation damage, and its knockdown or inhibition increases sensitivity to Temozolomide in glioblastoma and colorectal cancer cell lines[1].
[1]. Jack C Exell, et al. Cellularly Active N-hydroxyurea FEN1 Inhibitors Block Substrate Entry to the Active Site. Nat Chem Biol. 2016 Oct;12(10):815-21.