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505328 PARP Inhibitor Set II - Calbiochem

PARP Inhibitor Set II - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (R)- & (S)-& 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-(1-phenylethyl)propanamide, ME0328, ME0327, ARTD3 inhibitor, PARP3 Inhibitor, Poly-ADP-ribose Polymerase Inhibitor XVI

Primary Target: PARP3
505328
  
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₁₉N₃O₂
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®
Synonyms(R)- & (S)-& 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-(1-phenylethyl)propanamide, ME0328, ME0327, ARTD3 inhibitor, PARP3 Inhibitor, Poly-ADP-ribose Polymerase Inhibitor XVI
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
Global Trade Identification Number
Catalog Number GTIN
505328

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
Synonyms(R)- & (S)-& 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-(1-phenylethyl)propanamide, ME0328, ME0327, ARTD3 inhibitor, PARP3 Inhibitor, Poly-ADP-ribose Polymerase Inhibitor XVI
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 Protect from light
+2°C to +8°C
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.