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CAS No.: 824983-91-7

FEN1-IN-1 Catalog No. CSN20336

Synonyms: LNT 1;FEN1- N-1

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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技术信息

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^[2]. 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^[3]. 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^[4].
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.
参考文献

[1] Ward TA, McHugh PJ, Durant ST. Small molecule inhibitors uncover synthetic genetic interactions of human flap endonuclease 1 (FEN1) with DNA damage response genes. PLoS One. 2017 Jun 19;12(6):e0179278.
[2] Ba S, Zhang H, Lee JY, Wu H, Ye R, Huang D, Li T. Investigation of human flap structure-specific endonuclease 1 (FEN1) activity on primer-template models and exploration of a substrate-based FEN1 inhibitor. Bioorg Med Chem. 2016 May 1;24(9):1988-92. doi: 10.1016/j.bmc.2016.03.025. Epub 2016 Mar 14. PMID: 27020684.
[3] Exell JC, Thompson MJ, Finger LD, Shaw SJ, Debreczeni J, Ward TA, McWhirter C, Siöberg CL, Martinez Molina D, Abbott WM, Jones CD, Nissink JW, Durant ST, Grasby JA. Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site. Nat Chem Biol. 2016 Oct;12(10):815-21. doi: 10.1038/nchembio.2148. Epub 2016 Aug 15. PMID: 27526030; PMCID: PMC5348030.
[4] Ward TA, McHugh PJ, Durant ST. Small molecule inhibitors uncover synthetic genetic interactions of human flap endonuclease 1 (FEN1) with DNA damage response genes. PLoS One. 2017 Jun 19;12(6):e0179278. doi: 10.1371/journal.pone.0179278. PMID: 28628639; PMCID: PMC5476263.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0090 mL
- 15.0452 mL
- 30.0905 mL
- 5 mM
- 0.6018 mL
- 3.0090 mL
- 6.0181 mL
- 10 mM
- 0.3009 mL
- 1.5045 mL
- 3.0090 mL

技术信息

CAS号

824983-91-7

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H12N2O5S

运输

蓝冰

分子量

332.33

别名

LNT 1;FEN1- N-1

溶解度

DMSO	67.5 mg/mL (203.1 mM)
Water	insoluble

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