AG-14361 - CAS 328543-09-5
Catalog number: 328543-09-5
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
AG14361 is a PARP-1 inhibitor with Ki < 5 nmol/L. AG14361 is at least 1000-fold more potent than the benzamides. The IC50 for AG14361 is 29 nM in permeabilized SW620 cells and 14 nM in intact SW620 cells.
AG14361; AG-14361; AG 14361.
Canonical SMILES:
1.Fluorine-Mediated Editing of a G-Quadruplex Folding Pathway.
Dickerhoff J;Weisz K Chembiochem. 2018 May 4;19(9):927-930. doi: 10.1002/cbic.201800099. Epub 2018 Apr 14.
A (3+1)-hybrid-type G-quadruplex was substituted within its central tetrad by a single 2'-fluoro-modified guanosine. Driven by the anti-favoring nucleoside analogue, a novel quadruplex fold with inversion of a single G-tract and conversion of a propeller loop into a lateral loop emerges. In addition, scalar couplings across hydrogen bonds demonstrate the formation of intra- and inter-residual F⋅⋅⋅H8-C8 pseudo-hydrogen bonds within the modified quadruplexes. Alternative folding can be rationalized by the impact of fluorine on intermediate species on the basis of a kinetic partitioning mechanism. Apparently, chemical or other environmental perturbations are able to redirect folding of a quadruplex, possibly modulating its regulatory role in physiological processes.
2.ER stress in human hepatic cells treated with Efavirenz: mitochondria again.
Apostolova N;Gomez-Sucerquia LJ;Alegre F;Funes HA;Victor VM;Barrachina MD;Blas-Garcia A;Esplugues JV J Hepatol. 2013 Oct;59(4):780-9. doi: 10.1016/j.jhep.2013.06.005. Epub 2013 Jun 17.
BACKGROUND & AIMS: ;ER stress is associated with a growing number of liver diseases, including drug-induced hepatotoxicity. The non-nucleoside analogue reverse transcriptase inhibitor Efavirenz, a cornerstone of the multidrug strategy employed to treat HIV1 infection, has been related to the development of various adverse events, including metabolic disturbances and hepatic toxicity, the mechanisms of which remain elusive. Recent evidence has pinpointed a specific mitochondrial effect of Efavirenz in human hepatic cells. This study assesses the induction of ER stress by Efavirenz in the same model and the implication of mitochondria in this process.;METHODS: ;Primary human hepatocytes and Hep3B were treated with clinically relevant concentrations of Efavirenz and parameters of ER stress were studied using standard cell biology techniques.;RESULTS: ;ER stress markers, including CHOP and GRP78 expression (both protein and mRNA), phosphorylation of eIF2α, and presence of the spliced form of XBP1 were upregulated. Efavirenz also enhanced cytosolic Ca(2+) content and induced morphological changes in the ER suggestive of ER stress. This response was greatly attenuated in cells with altered mitochondrial function (Rho°).
3.Effects of ribavirin on severe fever with thrombocytopenia syndrome virus in vitro.
Shimojima M;Fukushi S;Tani H;Yoshikawa T;Fukuma A;Taniguchi S;Suda Y;Maeda K;Takahashi T;Morikawa S;Saijo M Jpn J Infect Dis. 2014;67(6):423-7.
Severe fever with thrombocytopenia syndrome (SFTS) is a disease with a high case fatality rate that is caused by infection with the recently identified tick-borne SFTS virus (SFTSV), for which there are no specific countermeasures. We examined the effects of ribavirin and mizoribine, which are nucleoside analogue drugs with broad antiviral activities, on SFTSV proliferation in vitro. When 3 cell lines were treated with these drugs before and during infection with a Chinese SFTSV strain, the 99% effective concentrations (EC99) of ribavirin were 19-64 μg/ml (78-262 μM); in contrast, the EC99 of mizoribine was >500 μg/ml (1,929 μM). Similar levels of inhibitory effects of ribavirin were observed with 4 Japanese SFTSV strains. However, when Vero cells were treated with ribavirin 3 days after inoculation, the inhibitory effect was dramatically decreased, indicating that ribavirin did not effectively reduce virus production in pre-infected cells. These results suggest that ribavirin could be used as post-exposure prophylaxis for the prevention of SFTS.
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CAS 328543-09-5 AG-14361

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