NU 1025A potent PARP-1 and Topo I inhibitor

NU 1025 (CAS 90417-38-2)

NU 1025 | CAS 90417-38-2 is rated 5.0 out of 5 by 1.
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Synonym: 8-Hydroxy-2-methylquinazoline-4-one
Application: A potent PARP-1 and Topo I inhibitor
CAS Number: 90417-38-2
Purity: >98%
Molecular Weight: 176.2
Molecular Formula: C9H8N2O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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NU 1025 is a potent PARP-1 (poly(ADP-ribose) polymerase; PARP) inhibitor that has demonstrated the ability to enhance the cytotoxicity of the DNA methylating compound MTIC (sc-211930), bleomycin, and γ-irradiaton. Studies have reported that NU 1025 is 40 to 50 times stronger than benzamide (sc-202494) and 3-aminobenzamide (sc-3501), increases DNA double-strand and single strand breaks, and has neuroprotective effects. Additionally, NU 1025 amplifies the cytotoxic effect of camptothecin (sc-200871), which is a topoisomerase I (Topo I) inhibitor.


References

1. Boulton, S., et al. 1995. Br. J. Cancer. 72: 849-856. PMID: 7547230
2. Bowman, K.J., et al. 1998. Br. J. Cancer. 78: 1269-1277. PMID: 9823965
3. Boulton, S., et al. 1999. Carcinogenesis. 20: 199-203. PMID: 10069454
4. Bowman, K.J., et al. 2001. Br. J. Cancer. 84: 106-112. PMID: 11139322
5. Kaundal, R.K., et al. 2006. Life Sci. 79: 2293-2302. PMID: 16935310

Physical State :
Solid
Solubility :
Soluble in DMSO (>20 mg/mL), 1eq. NaOH (100 mM), ethanol, ethyl acetate, and methanol. Insoluble in water.
Storage :
Store at -20° C
Melting Point :
>250° C (dec.)
Boiling Point :
345.42° C at 760 mmHg (Predicted)
Density :
1.43 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
Poly(ADP-ribose) polymerase (PARP): IC50 = 400 nM; ADP-ribosyltransferase: IC50 = 400 nM (mouse)
Ki Data :
Poly(ADP-ribose) polymerase (PARP): Ki= 48 nM
pK Values :
pKa: 9.08 (Predicted), pKb: 2.2 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
63306
MDL Number :
MFCD00942555
SMILES :
CC1=NC(=O)C2=C(N1)C(=CC=C2)O

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Certificate of Analysis

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NU 1025  Product Citations

See how others have used NU 1025. Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 26921193  Tepper, S. et al. 2016. Oncotarget. 7: 13197-208.

PMID: # 22204001  Davis, K. et al. 2012. Mol. Med. 18: 359-369.

PMID: # 20610652  Zerfaoui, M. et al. 2010. J. Immunol. 185: 1894-1902.

PMID: # 20802516  Salvati, E. et al. 2010. Oncogene. 29: 6280-6293.

PMID: # 9823965  Bowman, KJ. et al. 1998. Br. J. Cancer. 78: 1269-1277.

PMID: # 21607289  Kim, H. et al. 2011 Sep-Oct. Mol. Med. 17: 893-900.

Citations 1 to 6 of 6 total
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Rated 5 out of 5 by from Cie lar Cie lar-Pobuda, A. et al. (PubMed 22321899) used the PARP-1 inhibitor NU 1025 to demonstrate that PARP-1 inhibition induces a late increase in the level of reactive oxygen species in cells after ionizing radiation. -SCBT Publication Review
Date published: 2015-02-16
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