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NU1025

PARP-1 inhibitor
 
ALX-270-370-M005 5 mg 106.00 USD
 
ALX-270-370-M025 25 mg 332.00 USD
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A potent poly(ADP-ribose) polymerase 1 (PARP-1) inhibitor (IC50=400nM) that potentiates the cytotoxicity of various DNA-active agents, including the DNA-methylating compound MTIC, the DNA strand break-inducing drug temozolomide (Prod. No. ALX-420-044), topotecan (Prod. No. ALX-350-133), bleomycin (Prod. No. BML-AP302), and ionizing radiation effective in murine L1210 leukemia cells, CHO, and in a variety of human tumor cell lines.

Product Specification

Alternative Name:8-Hydroxy-2-methylquinazoline-4-one
 
Formula:C9H8N2O2
 
MW:176.2
 
CAS:90417-38-2
 
Purity:≥98% (HPLC)
 
Appearance:Off-white to purple solid.
 
Solubility:Soluble in DMSO (25mg/ml). This solution can be further diluted 1:100 in tissue culture medium before use.
 
Reconstitution:Reconstitute with DMSO.
 
Shipping:Ambient
 
Short Term Storage:-20°C
 
Long Term Storage:-20°C
 
Handling:Protect from light. Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C.
 
270-370
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270-370

Product Literature References

Disrupted ADP-ribose metabolism with nuclear Poly (ADP-ribose) accumulation leads to different cell death pathways in presence of hydrogen peroxide in procyclic Trypanosoma brucei: M. Schlesinger, et al.; Parasit. Vectors 9, 173 (2016), Application(s): Potency of inhibitors, Abstract; Full Text
Role of SIRT1 in homologous recombination: M. Uhl, et al.; DNA Repair (Amst) 9, 383 (2010), Abstract;
The properties of tumor-initiating cells from a hepatocellular carcinoma patient's primary and recurrent tumor: X.L. Xu, et al.; Carcinogenesis 31, 167 (2010), Abstract; Full Text
3-Methylindole is mutagenic and a possible pulmonary carcinogen: J.M. Weems, et al.; Toxicol. Sci. 112, 59 (2009), Abstract; Full Text
Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines: C.A. Delaney, et al.; Clin. Cancer Res. 6, 2860 (2000), Abstract; Full Text
Interactive effects of inhibitors of poly(ADP-ribose) polymerase and DNA-dependent protein kinase on cellular responses to DNA damage: S. Boulton, et al.; Carcinogenesis 20, 199 (1999), Abstract; Full Text
Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064: K.J. Bowman, et al.; Br. J. Cancer 78, 1269 (1998), Abstract;
Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP): R.J. Griffin, et al.; J. Med. Chem. 41, 5247 (1998), Abstract;
Nephron-sparing surgery for renal cell carcinoma: J.H. Griffin & R.C. Flanigan; Tech. Urol. 2, 43 (1996), Abstract;
Potentiation of temozolomide-induced cytotoxicity: a comparative study of the biological effects of poly(ADP-ribose) polymerase inhibitors: S. Boulton, et al.; Br. J. Cancer 72, 849 (1995), Abstract;

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Topotecan . hydrochloride 

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Bleomycin sulfate 

Antitumor antibiotic
9041-93-4, ≥98% (HPLC) | Print as PDF
 
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The PARP Family & ADP Ribosylation
The PARP Family & ADP Ribosylation
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