CAS:824983-91-7FEN1 Inhibitor C1

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FEN1 inhibitor C1 is an inhibitor of flap endonuclease 1 (FEN1) which is required for proficient DNA replication and the repair of DNA damage.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

824983-91-7

储存条件

分子式

C15H12N2O5S

运输

蓝冰

分子量

332.33

别名

溶解度

DMSO	67.5 mg/mL (203.1 mM)
Water	insoluble

动物实验配方

生物活性

描述Human flap structure-specific endonuclease 1 (FEN1), the prototypical member of the 5′ nuclease superfamily, has been known to play critical roles in DNA replication and DNA repair process in Eukaryotic cells. In vivo FEN1 is proved to cleave the 5' overhanging flap (primer) on lagging strand, generating nicked DNA duplex with a phosphate group attached to 5'-end. FEN1 inhibitor C1 is an inhibitor of FEN1. FEN1 Inhibitor C1 at high concentrations showed cytotoxic towards SW620 cells with an EC₅₀ of 11 μM. HCT-116 cells disrupted for MRE11A were more sensitive to a dose escalation of FEN1 inhibitor C1, and at 10 μM, 11% survival in the MRE11A deficient cell-line compared to 66% in the control cell-line were observed.
作用机制FEN1 Inhibitor C1 co-crystallizes within the active site of FEN1 in vitro, with inhibition achieved partly through the co-ordination of Mg²⁺ ions by the N-hydroxyurea moiety of FEN1 Inhibitor C1.