P1738
PARP-1 bovine
≥98% (SDS-PAGE), ≥300 U/mg, buffered aqueous glycerol solution
Synonym(s):
NAD+ ADP-ribosyltransferase, Poly(ADP-ribose) Polymerase, Poly(ADP-ribose) Synthetase
Assay
≥98% (SDS-PAGE)
form
buffered aqueous glycerol solution
specific activity
≥300 U/mg
UniProt accession no.
storage temp.
−70°C
Gene Information
cow ... ADPRT(286764)
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Biochem/physiol Actions
PARP-1, a nuclear enzyme that synthesizes ADP-ribose polymers from NAD, specifically binds Zn2+ and DNA, and recognizes single-strand breaks in DNA. It is involved in base excision repair, both short-patch and long-patch, rejoining DNA strand breaks and plays a role in p53 expression and activation. A high level of basal neuronal DNA damage and PARP activity has been reported in rat brain tissue. PARP-1 was shown to be required for HIV-1 integration into DNA. If PARP-1 is deficient there is no productive HIV-1 infection.
Physical form
Solution in 50 mM Tris-HCl, pH 7.4, containing 1 M NaCl and 10 mM β-mercaptoethanol.
Other Notes
One unit synthesizes 1 nmol of poly(ADP-ribose)/min at pH 7.5 at 25 °C.
Regulatory Information
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L Masuelli et al.
Journal of biological regulators and homeostatic agents, 27(1), 105-119 (2013-03-16)
Breast cancer is a leading cancer in women and despite the benefits of the current therapies a significant number of patients with this tumor is at risk of relapse. Some of the alterations taking place in breast cancer cells are
Ted Lau et al.
Cancer research, 73(10), 3132-3144 (2013-03-30)
Most colorectal cancers (CRC) are initiated by mutations of APC, leading to increased β-catenin-mediated signaling. However, continued requirement of Wnt/β-catenin signaling for tumor progression in the context of acquired KRAS and other mutations is less well-established. To attenuate Wnt/β-catenin signaling
Na Ye et al.
Journal of medicinal chemistry, 56(7), 2885-2903 (2013-03-12)
A series of benzo[de][1,7]naphthyridin-7(8H)-ones possessing a functionalized long-chain appendage have been designed and evaluated as novel PARP1 inhibitors. The initial effort led to the first-generation PARP1 inhibitor 26 bearing a terminal phthalazin-1(2H)-one framework and showing remarkably high PARP1 inhibitory activity
Sabine Mueller et al.
Anticancer research, 33(3), 755-762 (2013-03-14)
To assess poly (ADP-ribose) polymerase (PARP) inhibitor MK-4827 together with radiation for the treatment of neuroblastoma. Clonogenic survival assays were used to assess MK-4827, radiation and combination thereof in four neuroblastoma cell lines. In vivo efficacy was tested in a
Andrew Voronkov et al.
Journal of medicinal chemistry, 56(7), 3012-3023 (2013-03-12)
Tankyrases 1 and 2 (TNKS1/2) are promising pharmacological biotargets with possible applications for the development of novel anticancer therapeutics. A focused structure-activity relationship study was conducted based on the tankyrase inhibitor JW74 (1). Chemical analoging of 1 improved the 1,2,4-triazole
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