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Merck
모든 사진(1)

Key Documents

A4847

Sigma-Aldrich

Alsterpaullone

≥98% (HPLC), powder

동의어(들):

9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5)-one

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About This Item

실험식(Hill 표기법):
C16H11N3O3
CAS Number:
Molecular Weight:
293.28
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

분석

≥98% (HPLC)

형태

powder

저장 조건

desiccated

색상

yellow to brown

solubility

DMSO: ≥10 mg/mL

저장 온도

2-8°C

SMILES string

[O-][N+](=O)c1ccc2[nH]c-3c(CC(=O)Nc4ccccc-34)c2c1

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)

InChI key

OLUKILHGKRVDCT-UHFFFAOYSA-N

유전자 정보

애플리케이션

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.

생화학적/생리학적 작용

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.
Potent and selective inhibitor of GSK-3β and CDK5/p25; potent inhibitor of CDK1/cyclin B (IC50 = 0.035 μM).

특징 및 장점

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

개인 보호 장비

dust mask type N95 (US), Eyeshields, Gloves


시험 성적서(COA)

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문서 라이브러리 방문

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)

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