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AG-14361 , CAS 328543-09-5
AG-14361 , CAS 328543-09-5
Artikelnummer
BPS27602-3
Verpackungseinheit
50 mg
Hersteller
BPS Bioscience
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Background: A 17-hour exposure of A549 cells to 0.4 µM AG14361 does not change the expression of the 6800 genes. Thus, although 0.4 µM AG14361 inhibits cellular PARP-1 activity by more than 85%, it essentially does not change gene expression and cell proliferation, indicating that the cellular effects of this low concentration of AG14361 are specific for PARP-1 inhibition. Higher, growth-inhibitory concentrations of AG14361 affects gene expression, but these effects are not likely to be related to PARP-1 inhibition because cell proliferation is affected equally in PARP-/- and PARP-1+/+ cells.
Biological Activity: The IC50 for AG14361 is 29 nM in permeabilized SW620 cells and 14 nM in intact SW620 cells.
CAS Number: 328543-09-5
Description: AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.
Purity: ≥98% by HPLC
Solubility: Soluble in DMSO. Solubility in water or ethanol is <1 mg/ml
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: PARP1
Biosafety Level: Not applicable (BSL-1)
References: 1. Smith LM, et al. Clin Cancer Res. 2005 Dec 1;11(23):8449-57.
2. Curtin NJ, et al. Clin Cancer Res. 2004 Feb 1;10(3):881-9.
3. Calabrese CR, et al. J Natl Cancer Inst. 2004 Jan 7;96(1):56-67.
Background: A 17-hour exposure of A549 cells to 0.4 µM AG14361 does not change the expression of the 6800 genes. Thus, although 0.4 µM AG14361 inhibits cellular PARP-1 activity by more than 85%, it essentially does not change gene expression and cell proliferation, indicating that the cellular effects of this low concentration of AG14361 are specific for PARP-1 inhibition. Higher, growth-inhibitory concentrations of AG14361 affects gene expression, but these effects are not likely to be related to PARP-1 inhibition because cell proliferation is affected equally in PARP-/- and PARP-1+/+ cells.
Biological Activity: The IC50 for AG14361 is 29 nM in permeabilized SW620 cells and 14 nM in intact SW620 cells.
CAS Number: 328543-09-5
Description: AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least 1000-fold more potent than the benzamides. AG14361 treatment before irradiation statistically significantly increases the sensitivity to radiation therapy. AG14361 enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons and increases the persistence of camptothecin-induced DNA single-strand breaks.
Purity: ≥98% by HPLC
Solubility: Soluble in DMSO. Solubility in water or ethanol is <1 mg/ml
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: PARP1
Biosafety Level: Not applicable (BSL-1)
References: 1. Smith LM, et al. Clin Cancer Res. 2005 Dec 1;11(23):8449-57.
2. Curtin NJ, et al. Clin Cancer Res. 2004 Feb 1;10(3):881-9.
3. Calabrese CR, et al. J Natl Cancer Inst. 2004 Jan 7;96(1):56-67.
| Artikelnummer | BPS27602-3 |
|---|---|
| Hersteller | BPS Bioscience |
| Hersteller Artikelnummer | 27602-3 |
| Green Labware | Nein |
| Verpackungseinheit | 50 mg |
| Mengeneinheit | STK |
| Produktinformation (PDF) | Download |
| MSDS (PDF) |
|
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Gernot Ensinger, M.Sc.
Laurent Haze
