A4847
アルスターパウロン
≥98% (HPLC), GSK-3β and CDK5/p25 inhibitor, powder
別名:
9-ニトロ-7,12-ジヒドロインドロ-[3,2-d][1]ベンゾアゼピン-6(5)-オン
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この商品について
実験式（ヒル表記法）:
C16H11N3O3
CAS番号:
分子量:
293.28
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
製品名
アルスターパウロン, ≥98% (HPLC), powder
SMILES string
[O-][N+](=O)c1ccc2[nH]c-3c(CC(=O)Nc4ccccc-34)c2c1
InChI key
OLUKILHGKRVDCT-UHFFFAOYSA-N
InChI
1S/C16H11N3O3/c20-15-8-12-11-7-9(19(21)22)5-6-14(11)18-16(12)10-3-1-2-4-13(10)17-15/h1-7,18H,8H2,(H,17,20)
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
yellow to brown
solubility
DMSO: ≥10 mg/mL
storage temp.
2-8°C
Quality Level
Gene Information
rat ... Gsk3b(84027)
Biochem/physiol Actions
GSK-3βおよびCDK5/p25の強力かつ選択的なインヒビタ-です。また、CDK1/サイクリンBの強力なインヒビタ-です(IC50= 0.035μM)。
Alsterpaullone (ALP) is a cyclin-dependent kinase (CDK) inhibitor. It is considered as a therapeutic agent for group 3 medulloblastomas. Alsterpaullone modulates the progression of cell cycle. It can arrest cell cycle and stimulate the apoptosis of cancer cells by activating caspase-9 through perturbation of mitochondrial membrane potential.
Application
Alsterpaullone has been used to stabilize β-catenin.
Alsterpaullone inhibits GSK-3β, CDK5/p25, and CDK1/cyclin B. Alsterpaullone has also been studied as an antimanic therapeutic for the acute manic phase of bipolar disorder.
Features and Benefits
This compound is featured on the CDKs and GSK-3 pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
Michael Trevino et al.
Developmental dynamics : an official publication of the American Association of Anatomists, 240(12), 2673-2679 (2011-11-05)
Although regeneration is widespread among metazoa, the molecular mechanisms have been studied in only a handful of taxa. Of these taxa, fewer still are amenable to studies of embryogenesis. Our understanding of the evolution of regeneration, and its relation to
Tsuneo Takadera et al.
Neurotoxicity research, 21(3), 309-316 (2011-10-19)
In the central nervous system, members of the Src family of tyrosine kinases (SFKs) are widely expressed and are abundant in neurons. The purpose of this study is to examine whether glycogen synthase-3 (GSK-3) is involved in SFK inhibitor-induced apoptosis.
Mikhail Kalinichev et al.
The international journal of neuropsychopharmacology, 14(8), 1051-1067 (2011-01-07)
There is a growing body of evidence suggesting that animal models can be developed to probe the specific domains of bipolar disorder (BD) using the endophenotype approach. Here we tested clinically active antimanic drugs to validate amphetamine-induced hyperactivity in Black
C Schultz et al.
Journal of medicinal chemistry, 42(15), 2909-2919 (1999-07-30)
The paullones represent a novel class of small molecule cyclin-dependent kinase (CDK) inhibitors. To investigate structure-activity relationships and to develop paullones with antitumor activity, derivatives of the lead structure kenpaullone (9-bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, 4a) were synthesized. Paullones with different substituents in the
Identification of alsterpaullone as a novel small molecule inhibitor to target group 3 medulloblastoma
Faria C C, et al.
Testing, 6(25), 21718-21718 (2015)
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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