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KU-0058948 hydrochloride
- Parent CAS: 763111-49-5
- Soluble in water and DMSO
- MF: C21H21FN4O2.HCl
- MW: 416.88
Description
KU-0058948 hydrochloride is a potent and selective poly(ADP-ribose) polymerase 1 (PARP1) inhibitor with an IC50 value of 3.4 nM. By inhibiting PARP1-mediated DNA repair, KU-0058948 serves as a valuable tool for investigating DNA damage response pathways and PARP-dependent cellular processes.
PARP1 is a key enzyme involved in DNA damage detection and repair, particularly in the repair of single-strand DNA breaks. Pharmacological inhibition of PARP1 has become an important strategy for studying DNA repair mechanisms, genome stability, and synthetic lethality in cancer. In addition to PARP inhibition, KU-0058948 activates extracellular signal-regulated kinase 8 (ERK8/MAPK15) in cells and induces cell cycle arrest and apoptosis in primary myeloid leukemic cells and myeloid leukemia cell lines. KU-0058948 is therefore a useful tool for DNA repair, cancer biology, and leukemia research.
Key Features
- Potent and selective PARP1 inhibitor
- IC50: 3.4 nM for PARP1
- Inhibits PARP-mediated DNA repair pathways
- Activates ERK8 (MAPK15) signaling in cells
- Induces cell cycle arrest and apoptosis in leukemia models
Applications
- PARP1 and DNA repair research
- DNA damage response studies
- Cancer biology and synthetic lethality investigations
- Leukemia and hematologic malignancy research
- Cell cycle regulation and apoptosis studies
More Information
| Parent CAS No. | 763111-49-5 |
|---|---|
| Chemical Name | 4-(3-(1,4-diazepane-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one hydrochloride |
| SMILES | C1(=O)C2=C(C=CC=C2)C(CC2=CC=C(F)C(C(N3CCCNCC3)=O)=C2)=NN1.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C21H21FN4O2.ClH/c22-18-7-6-14(12-17(18)21(28)26-10-3-8-23-9-11-26)13-19-15-4-1-2-5-16(15)20(27)25-24-19;/h1-2,4-7,12,23H,3,8-11,13H2,(H,25,27);1H |
| InChiKey | GXROJFUSWNEBPH-UHFFFAOYSA-N |
| CID | 91826495 |
| Short Description | PARP1 inhibitor |
References
- H Farmer et al. Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy. Nature 2005, 434, 917-921.
- K Ratnam and JA Low. Current Development of Clinical Inhibitors of Poly(ADP-Ribose) Polymerase in Oncology. Clin. Cancer Res. 2007, 13, 1383.
- NC Turner et al. A synthetic lethal siRNA screen identifying genes mediating sensitivity to a PARP inhibitor. EMBO J. 2008, 27, 1368-1377.
- T Hay et al. Poly(ADP-ribose) polymerase-1 inhibitor treatment regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin. Cancer Res. 2009, 69(9), 3850.
- List of publications using KU-0058948 (Axon 2001) purchased from Axon Medchem
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