All Photos(1)
2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, AG 14361, AG-14361
C19H20N4O
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
SMILES string
O=C1C2=C3C(N=C(N3CCN1)C4=CC=C(C=C4)CN(C)C)=CC=C2
InChI
1S/C19H20N4O/c1-22(2)12-13-6-8-14(9-7-13)18-21-16-5-3-4-15-17(16)23(18)11-10-20-19(15)24/h3-9H,10-12H2,1-2H3,(H,20,24)
InChI key
SEKJSSBJKFLZIT-UHFFFAOYSA-N
Biochem/physiol Actions
AG14361 is a potent oly(ADP-ribose) polymerase-1 inhibitor (human PARP-1 Ki = 5.8 nM) that suppresses 25 μM MNNG-induced PARP-1 activity (NAD+ depletion = 70% without vs.12% with 0.4 μM AG14361; 87% reduced ADP-ribose polymer induction with 0.4 μM AG14361) and greatly amplifies temozolomide and topotecan cytotoxicity (2.2- and 2.0-fold lower IG50, respectively, with 0.4 μM AG14361) in A549 cultures. AG14361 is shown to selectively kill BRCA2-deficient cells over BRCA2-expressing cells both in cultures (1-10 μM) and in mice in vivo (25 mg/10 mL/kg/d ip).
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Scientific reports, 8(1), 3664-3664 (2018-02-28)
Despite continuous improvements in treatment of glioblastoma, tumor recurrence and therapy resistance still occur in a high proportion of patients. One underlying reason for this radioresistance might be the presence of glioblastoma cancer stem cells (GSCs), which feature high DNA
Acta pharmacologica Sinica, 40(5), 589-598 (2018-07-22)
High-mobility group box 1 (HMGB1) exhibits various functions according to its subcellular location, which is finely conditioned by diverse post-translational modifications, such as acetylation. The nuclear HMGB1 may prevent from cardiac hypertrophy, whereas its exogenous protein is proven to induce
Scientific reports, 9(1), 10219-10219 (2019-07-17)
Resveratrol (RSV) and nicotinamide (NAM) have garnered considerable attention due to their anti-inflammatory and anti-aging properties. NAM is a transient inhibitor of class III histone deacetylase SIRTs (silent mating type information regulation 2 homologs) and SIRT1 is an inhibitor of
Journal of medicinal chemistry, 46(2), 210-213 (2003-01-10)
Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. Several compounds were found to be powerful chemopotentiators of temozolomide and topotecan in both A549 and LoVo cell lines. In vitro inhibition of PARP-1 was confirmed by direct measurement
JCI insight, 4(12) (2019-06-21)
The activation and recruitment of NK cells to the site of viral infection are crucial for virus control. However, it remains largely unknown what controls the recruitment of the activated NK cells to the infection site. In a model of
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service