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Merck
CN

SML3081

AG14361

≥98% (HPLC)

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C19H20N4O
CAS Number:
328543-09-5
Molecular Weight:
320.39
MDL number:
MFCD18385009
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Quality Level

100

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).
Potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor in vitro and in vivo.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000129742
0000129744
0000127991

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Qiyang Shou et al.
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
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
Sandra M Martín-Guerrero et al.
PloS one, 12(10), e0187130-e0187130 (2017-10-27)
Poly(ADP-ribose)polymerases (PARPs) are a family of NAD+ consuming enzymes that play a crucial role in many cellular processes, most clearly in maintaining genome integrity. Here, we present an extensive analysis of the alteration of mitochondrial morphology and the relationship to
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