505328 | PARP Inhibitor Set II - Calbiochem

505328
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉H₁₉N₃O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.05328.0001
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          Glass bottle 1 set
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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
          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.