For research purposes only

Cat. No BA120188000

Availability - 10 mg in stock
- larger amount can be synthesized in 8 weeks

Description of biological activity

Selective Poly(ADP-Ribose) Polymerase-1 (PARP-1) inhibitor. The compound showed IC50 5 nmol/l for human PARP-1 [Bioorg. Med. Chem. Lett. 2005, 15, 2235-2238]. Cytotoxic to human colon cancer RKO cells, human lung cancer A549 cells, human lung cancer A549 cells at 100 μmol/l [Proc. Nat. Acad. Sci. USA 2010, 107, 2201-2206].

Keywords: Anti-cancer

TECHNICAL INFORMATION

KU0058684, 1-[2-fluoro-5-(4-oxo-3,4-dihydrophthalazin-1-ylmethyl)phenyl]pyrrolidine-2,5-dione selective Poly(ADP-Ribose) Polymerase-1 (PARP-1) inhibitor.

IUPAC Name: KU0058684, 1-[2-fluoro-5-(4-oxo-3,4-dihydrophthalazin-1-ylmethyl)phenyl]pyrrolidine-2,5-dione

CAS Number: 623578-11-0

Purity: > 96% chemical purity (LCMS)

REFERENCES

1. Nature 2005, 434, 917-21
2. Cancer Res. 2006, 66, 8109-15

Latest added compounds

5-(4-Hydroxy-4-methyl-isoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-(3-methyl-5-trifluoromethyl-1H-pyrazol-4-ylmethyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione

Selective inhibitor of MCT1 with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. Both lactate transport and cell growth are potently inhibited.

Anti-cancer

Inhibitors

 
5-(4-chlorophenyl)-N-{[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl}pyridine-3-carboxamide

selective inhibitor of Nav1.8 sodium channel (IC50 = 3 nM); for TRPV1, P2X2/3, Cav2.2 calcium channels, KCNQ2/3 potassium channels IC50 >10 µM

Analgesic

Inhibitors

 
1-[4-chloro-3-(trifluoromethyl)benzenesulfonyl]-4-[4-(5-methyl-1H-pyrazol-1-yl)benzoyl]piperazine

inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smuf1)

Bone disorders

Inhibitors