AG-14361

Catalog #

27602-1

$205 *

Size: 5 mg

Qty

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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.

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Synonyms

1-(4-((dimethylamino)methyl)phenyl)-8,9-dihydro-2,7,9a-triazabenzo[cd]azulen-6(7H)-one

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Product Data Gallery

Product Info

Storage and Usage

Citations

Purity

≥98% by HPLC

Target(s)

PARP1

Formula

C₁₉H₂₀N₄O

320.4 Da

Solubility

Soluble in DMSO. Solubility in water or ethanol is <1 mg/ml

Biological Activity

The IC50 for AG14361 is 29 nM in permeabilized SW620 cells and 14 nM in intact SW620 cells.

CAS Registry #

328543-09-5

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.

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.

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