SML3081
AG14361
≥98% (HPLC)
别名:
2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, AG 14361, AG-14361
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选择尺寸
关于此项目
经验公式（希尔记法）:
C19H20N4O
化学文摘社编号:
分子量:
320.39
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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)
SMILES string
O=C1C2=C3C(N=C(N3CCN1)C4=CC=C(C=C4)CN(C)C)=CC=C2
InChI key
SEKJSSBJKFLZIT-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
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).
Potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor in vitro and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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JCI insight, 4(12) (2019-06-21)
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Donald J Skalitzky et al.
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
Qian Li et al.
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
Paul Lesueur et al.
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
Helen E Bryant et al.
Nature, 434(7035), 913-917 (2005-04-15)
Poly(ADP-ribose) polymerase (PARP1) facilitates DNA repair by binding to DNA breaks and attracting DNA repair proteins to the site of damage. Nevertheless, PARP1-/- mice are viable, fertile and do not develop early onset tumours. Here, we show that PARP inhibitors
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