126870
Alsterpaullone
A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC₅₀ = 4 nM) and Cdk1/cyclin B (IC₅₀ = 35 nM).
别名:
Alsterpaullone, 9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, 9-Nitropaullone, NSC 705701
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
light yellow to brown
溶解性
DMSO: 20 mg/mL
运输
ambient
储存温度
−20°C
SMILES字符串
[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 key
OLUKILHGKRVDCT-UHFFFAOYSA-N
一般描述
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
GSK-3β, Cdk1/cyclin B
Product competes with ATP.
Reversible: yes
Target IC50: 4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively
包装
Packaged under inert gas
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Leost, M., et al. 2000. Eur. J. Biochem.267, 5983.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
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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