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505328 PARP Inhibitor Set II - Calbiochem

505328
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₉H₁₉N₃O₂

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      Description
      OverviewA cell-permeable, non-toxic, 4-oxo-3H-quinazolin derivative that acts as a highly potent and specific inhibitor of ADP-ribosyltransferase diphtheria toxin-like 3 (ARTD3/PARP3, IC50 = 890 pM) that targets its nicotinamide binding site, with >7-fold selectivity over ARTD1 (IC50 = 6.3 µM) and >12-fold selectivity over ARTD2 (IC50 = 10.8 µM), and without observable activities for the rest of 11 ARTDs profiled (IC50 >30 µM). Shown to elicit a concentration dependent retention of γH2AX containing foci in A549 cells following g-irradiation-induced DNA damage. A negative control enantiomer ME0327 that is inactive for ARTD3 is also included.
      Catalogue Number505328
      Brand Family Calbiochem®
      SynonymsARTD3 inhibitor, PARP3 Inhibitor, Poly-ADP-ribose Polymerase Inhibitor XVI, (R)- & (S)-& 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-(1-phenylethyl)propanamide, ME0328, ME0327
      References
      ReferencesLindgren, A., et al, 2013, ACS Chem. Biol. 8, 1698.
      Product Information
      FormSolid
      Formulation1 set consists of 5 MG PARP Inhibitor XVI, PARP3-Selective, ME0328 (Cat. No. 505329) and 5 MG ME0327, Negative Control (Cat. No. 505330).
      Hill FormulaC₁₉H₁₉N₃O₂
      Chemical formulaC₁₉H₁₉N₃O₂
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPARP3
      Primary Target IC<sub>50</sub>890pM
      Purity≥99% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      References

      Reference overview
      Lindgren, A., et al, 2013, ACS Chem. Biol. 8, 1698.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision15-November-2013 JSW
      SynonymsARTD3 inhibitor, PARP3 Inhibitor, Poly-ADP-ribose Polymerase Inhibitor XVI, (R)- & (S)-& 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-(1-phenylethyl)propanamide, ME0328, ME0327
      DescriptionA cell-permeable, 4-oxo-3H-quinazolin derivative whose (S) enantiomer, ME0328, acts as an active site-targeting, ADP-ribosyltransferase diphtheria toxin-like 3/ARTD3/PARP3-selective inhibitor (IC50 = 890 nM), while exhibiting much reduced or little activity against ARTD1/2/4/5/6/7/8/10/12/15 (IC50 >30 µM). Effectively delays cellular DNA repair following γ-irradiation (2 Gy) in human alveolar basal epithelial A549 and primary fetal lung fibrolast MRC5 cultures (1 h pretreatment at 0.1 to 30 µM prior to IR) with no detectable cytotoxicity up to 72 h at 10 µM. The inactive (R) enantiomer, ME0327, is also included.
      FormSolid
      Formulation1 set consists of 5 MG PARP Inhibitor XVI, PARP3-Selective, ME0328 (Cat. No. 505329) and 5 MG ME0327, Negative Control (Cat. No. 505330).
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₉H₁₉N₃O₂
      Purity≥99% by HPLC
      SolubilityEach compound is soluble at 25 mg/ml in DMSO.
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesLindgren, A., et al, 2013, ACS Chem. Biol. 8, 1698.