ME0328

PARP inhibitor,potent and selective CAS# 1445251-22-8

ME0328

Catalog No. BCC3995----Order now to get a substantial discount!

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Quality Control of ME0328

Number of papers citing our products

Chemical structure

ME0328

3D structure

Chemical Properties of ME0328

Cas No. 1445251-22-8 SDF Download SDF
PubChem ID 71571526 Appearance Powder
Formula C19H19N3O2 M.Wt 321.37
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 75 mg/mL (233.38 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 3-(4-oxo-1H-quinazolin-2-yl)-N-[(1S)-1-phenylethyl]propanamide
SMILES CC(C1=CC=CC=C1)NC(=O)CCC2=NC(=O)C3=CC=CC=C3N2
Standard InChIKey QIHBWVVVRYYYRO-ZDUSSCGKSA-N
Standard InChI InChI=1S/C19H19N3O2/c1-13(14-7-3-2-4-8-14)20-18(23)12-11-17-21-16-10-6-5-9-15(16)19(24)22-17/h2-10,13H,11-12H2,1H3,(H,20,23)(H,21,22,24)/t13-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ME0328

DescriptionInhibitor of PARP-3 (IC50 = 0.89 μM). Displays selectivity for PARP-3 over PARP-1, PARP-2 and other ARDT enzymes (IC50 values are 6.3, 10.8 and >30 μM respectively). Enhances CRISPR-Cas9-mediated HER2 mutation frequency, resulting in increased reduction in proliferation of HER2-positive breast cancer cells. Cell permeable.

ME0328 Dilution Calculator

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ME0328 Molarity Calculator

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Preparing Stock Solutions of ME0328

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1117 mL 15.5584 mL 31.1168 mL 62.2336 mL 77.792 mL
5 mM 0.6223 mL 3.1117 mL 6.2234 mL 12.4467 mL 15.5584 mL
10 mM 0.3112 mL 1.5558 mL 3.1117 mL 6.2234 mL 7.7792 mL
50 mM 0.0622 mL 0.3112 mL 0.6223 mL 1.2447 mL 1.5558 mL
100 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.6223 mL 0.7779 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on ME0328

ME0328 is a potent and selective inhibitor of PARP with IC50 value of 0.89 and 6.3 μM for PARP3 and PARP1, respectively [1].

Poly (ADP-ribose) polymerase (PARP) is a family of proteins mainly involved in programmed cell death and DNA repair. The overactivation of PARP may reduce the stores of cellular NAD+ and induce ATP depletion and cell death.

ME0328 is a potent and selective PARP inhibitor. ME0328 selectively inhibited ADP-ribosyltransferase-3/poly(ADP-ribose) polymerase-3 (ARTD3) with IC50 value of 0.89 μM and inhibited ARTD1 and ARTD2 with IC50 values of 6.3 and 10.8 μM, respectively. In human alveolar basal epithelial (A549) cells, treatment with ME0355 (10 μM) followed by γ-irradiation significantly delayed γH2AX-foci resolution in a concentration-dependent way, which suggested that ME0328 inhibited ARTD3 in cells. In nonirradiated human A549 and mouse MRC5 cells, ME0328 (10 μM) did not exhibit toxicity [1].

Reference:
[1].  Lindgren AE, Karlberg T, Thorsell AG, et al. PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3. ACS Chem Biol, 2013, 8(8): 1698-1703.

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References on ME0328

PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3.[Pubmed:23742272]

ACS Chem Biol. 2013 Aug 16;8(8):1698-703.

Inhibiting ADP-ribosyl transferases with PARP-inhibitors is considered a promising strategy for the treatment of many cancers and ischemia, but most of the cellular targets are poorly characterized. Here, we describe an inhibitor of ADP-ribosyltransferase-3/poly(ADP-ribose) polymerase-3 (ARTD3), a regulator of DNA repair and mitotic progression. In vitro profiling against 12 members of the enzyme family suggests selectivity for ARTD3, and crystal structures illustrate the molecular basis for inhibitor selectivity. The compound is active in cells, where it elicits ARTD3-specific effects at submicromolar concentration. Our results show that by targeting the nicotinamide binding site, selective inhibition can be achieved among the closest relatives of the validated clinical target, ADP-ribosyltransferase-1/poly(ADP-ribose) polymerase-1.

CRISPR-mediated targeting of HER2 inhibits cell proliferation through a dominant negative mutation.[Pubmed:27815036]

Cancer Lett. 2017 Jan 28;385:137-143.

With the discovery of the CRISPR/Cas9 technology, genome editing could be performed in a rapid, precise and effective manner. Its potential applications in functional interrogation of cancer-causing genes and cancer therapy have been extensively explored. In this study, we demonstrated the use of the CRISPR/Cas9 system to directly target the oncogene HER2. Directing Cas9 to exons of the HER2 gene inhibited cell growth in breast cancer cell lines that harbor amplification of the HER2 locus. The inhibitory effect was potentiated with the addition of PARP inhibitors. Unexpectedly, CRISPR-induced mutations did not significantly affect the level of HER2 protein expression. Instead, CRISPR targeting appeared to exert its effect through a dominant negative mutation. This HER2 mutant interfered with the MAPK/ERK axis of HER2 downstream signaling. Our work provides a novel mechanism underlying the anti-cancer effects of HER2-targeting by CRISPR/Cas9, which is distinct from the clinical drug Herceptin. In addition, it opens up the possibility that incomplete CRISPR targeting of certain oncogenes could still have therapeutic value by generation of dominant negative mutants.

Description

ME0328 is a potent and selective ARTD3/PARP3 inhibitor with an IC50 of 0.89±0.28 μM.

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