| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | FEN1-IN-3 | ||||||||||||
| CAS | 2109805-87-8 | ||||||||||||
| Formula | C15H12N2O4 | ||||||||||||
| Molar Mass | 284.27 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. |
FEN1-IN-3
CAS: 2109805-87-8 F: C15H12N2O4 W: 284.27
FEN1-IN-3 (Compound 4) is a human flap endonuclease-1 (hFEN1) inhibitor. FEN1-IN-3 stabilizes hFEN1 with an EC50 of 6.8
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