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 Details
| Alternative Name: | 8-Hydroxy-2-methylquinazoline-4-one |
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| Formula: | C9H8N2O2 |
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| MW: | 176.2 |
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| CAS: | 90417-38-2 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | Off-white to purple solid. |
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| Solubility: | Soluble in DMSO (25mg/ml). This solution can be further diluted 1:100 in tissue culture medium before use. |
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| Reconstitution: | Reconstitute with DMSO. |
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| Shipping: | Ambient |
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| Short Term Storage: | -20°C |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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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;
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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;
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3-Methylindole is mutagenic and a possible pulmonary carcinogen: J.M. Weems, et al.; Toxicol. Sci.
112, 59 (2009),
Abstract;
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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;
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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;
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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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