Alsterpaullone

Name: Alsterpaullone
Brand: MM

A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC₅₀ = 4 nM) and Cdk1/cyclin B (IC₅₀ = 35 nM).

同義詞:

Alsterpaullone, 9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, 9-Nitropaullone, NSC 705701

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關於此項目

經驗公式（希爾表示法）:

C₁₆H₁₁N₃O₃

CAS 編號:

237430-03-4

分子量：:

293.28

MDL號碼:

MFCD02683579

分類程式碼代碼:

12352200

NACRES:

NA.77

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品質等級

100

化驗

≥95% (HPLC)

形狀

solid

製造商／商標名

Calbiochem^®

儲存條件

OK to freeze
protect from light

顏色

light yellow to brown

溶解度

DMSO: 20 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

SMILES 字串

[N+](=O)([O-])c1cc2c([nH]c3c2CC(=O)Nc4c3cccc4)cc1

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 密鑰

OLUKILHGKRVDCT-UHFFFAOYSA-N

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本產品	A4847	528111	217714
Sigma-Aldrich 126870 Alsterpaullone	Sigma-Aldrich A4847 阿特波龙	Sigma-Aldrich 528111 PI 3-Kα Inhibitor IV	Sigma-Aldrich 217714 5-氨基-3-（（4 -（氨基磺酰基）苯基）氨基）-N-（2，6-二氟苯基）-1H-1,2，4-三唑-1-硫代乙酰胺
assay ≥95% (HPLC)	assay ≥98% (HPLC)	assay ≥95% (HPLC)	assay ≥95% (HPLC)
form solid	form powder	form solid	form solid
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
manufacturer/tradename Calbiochem^®	manufacturer/tradename -	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®
storage temp. −20°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: 20 mg/mL	solubility DMSO: ≥10 mg/mL	solubility DMSO: 10 mg/mL	solubility DMSO: 10 mg/mL, THF: soluble, acetone: soluble

一般說明

A cell-permeable, potent, reversible, and ATP competitive inhibitor of cdk1/cyclin B (IC₅₀ = 35 nM) and GSK-3β (IC₅₀ = 4 nM). One of the most active paullones that acts by competing with ATP for binding to GSK-3β and inhibits the phosphorylation of tau. Also inhibits the activity of Cdk5/p25-dependent phosphorylation of DARPP-32 (a 32 kDa dopamine and adenosine 3′,5′-monophosphate-regulated phosphoprotein). Displays remarkable antitumor activity in vitro. Inhibits growth of the colon cancer cell line HCT-116, with an IC₅₀ in the nanomolar range.

生化／生理作用

Cell permeable: yes

Primary Target
GSK-3β, Cdk1/cyclin B

Product competes with ATP.

Reversible: yes

Target IC₅₀: 4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively

包裝

Packaged under inert gas

準備報告

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Leost, M., et al. 2000. Eur. J. Biochem.267, 5983.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免責聲明

Toxicity: Standard Handling (A)

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

分析證明 (COA)

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Preventing erosion of X-chromosome inactivation in human embryonic stem cells.

Marissa Cloutier et al.

Nature communications, 13(1), 2516-2516 (2022-05-07)

X-chromosome inactivation is a paradigm of epigenetic transcriptional regulation. Female human embryonic stem cells (hESCs) often undergo erosion of X-inactivation upon prolonged culture. Here, we investigate the sources of X-inactivation instability by deriving new primed pluripotent hESC lines. We find

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