2108829-86-1
Chemical Structure
KU-0058948 hydrochloride
- CAS No.: 2108829-86-1
- Formula:C21H22ClFN4O2
- Molecular Weight:416.88
IUPAC Name: 4-(3-(1,4-diazepane-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one hydrochloride
InChIKey: GXROJFUSWNEBPH-UHFFFAOYSA-N
SMILES: O=C1NN=C(CC2=CC=C(F)C(C(N3CCNCCC3)=O)=C2)C4=C1C=CC=C4.[H]Cl
Biological Activity: KU-0058948 hydrochloride is a potent PARP1 inhibitor with an IC50 of 3.4 nM. KU-0058948 hydrochloride induces the accumulation of DNA double-strand breaks through inhibition of PARP1, triggering chromosomal aberrations, cell cycle arrest, and apoptosis in homologous recombination-deficient cells, while impeding the recruitment of the NuRD/PcG complex to affect chromatin remodeling. KU-0058948 hydrochloride can be used for research on cancers such as myeloid leukemia[1][2][2][3][4][5][6][7][8][9].
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KU-0058948 hydrochloride | KU-0058948 hydrochloride is a potent PARP1 inhibitor with an IC50 of 3.4 nM. KU-0058948 hydrochloride induces the accumulation of DNA double-strand breaks through inhibition of PARP1, triggering chromosomal aberrations, cell cycle arrest, and apoptosis in homologous recombination-deficient cells, while impeding the recruitment of the NuRD/PcG complex to affect chromatin remodeling. KU-0058948 hydrochloride can be used for research on cancers such as myeloid leukemia. | |||||||||||||||||||||
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References
- [1]. Farmer H, et al. Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy. Nature. 2005 Apr 14;434(7035):917-21. [Content Brief]
- [2]. Gaymes TJ, et al. Inhibitors of poly ADP-ribose polymerase (PARP) induce apoptosis of myeloid leukemic cells: potential for therapy of myeloid leukemia and myelodysplastic syndromes. Haematologica. 2009 May;94(5):638-46. [Content Brief]
- [3]. Luijsterburg MS, et al. DDB2 promotes chromatin decondensation at UV-induced DNA damage. The Journal of cell biology. 2012 Apr 16;197(2):267-81.
- [4]. Chou DM, et al. A chromatin localization screen reveals poly (ADP ribose)-regulated recruitment of the repressive polycomb and NuRD complexes to sites of DNA damage. Proceedings of the National Academy of Sciences of the United States of America. 2010 Oct 26;107(43):18475-80.
- [5]. Boetefuer EL, et al. Poly(ADP-ribose) polymerase 1 (PARP1) promotes oxidative stress-induced association of Cockayne syndrome group B protein with chromatin. The Journal of biological chemistry. 2018 Nov 16;293(46):17863-17874.
- [6]. Gaymes TJ, et al. Microsatellite instability induced mutations in DNA repair genes CtIP and MRE11 confer hypersensitivity to poly (ADP-ribose) polymerase inhibitors in myeloid malignancies. Haematologica. 2013 Sep;98(9):1397-406.
- [7]. Parameswaran B, et al. Damage-induced BRCA1 phosphorylation by Chk2 contributes to the timing of end resection. Cell cycle (Georgetown, Tex.). 2015;14(3):437-48.
- [8]. Slade D, et al. The structure and catalytic mechanism of a poly(ADP-ribose) glycohydrolase. Nature. 2011 Sep 04;477(7366):616-20. [Content Brief]
- [9]. Boehler C, et al. Poly(ADP-ribose) polymerase 3 (PARP3), a newcomer in cellular response to DNA damage and mitotic progression. Proceedings of the National Academy of Sciences of the United States of America. 2011 Feb 15;108(7):2783-8. [Content Brief]
