同义名 :	9-Nitropaullone; NSC 705701; Alp
	CAS号 :	237430-03-4
	货号 :	A310955
	分子式 :	C16H11N3O3
	纯度 :	99%+
	分子量 :	293.28
	MDL号 :	MFCD02683579
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	The cyclin-dependent protein kinases (CDKs) are protein-serine/threonine kinases that play crucial roles in regulation of cell cycle and transcription[1]. Glycogen synthase kinase-3 (GSK-3) is a cytoplasmic serine/threonine protein kinase that phosphorylates and inhibits glycogen synthase, thereby inhibiting glycogen synthesis from glucose[2]. Alsterpaullone (9-Nitropaullone; NSC 705701) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. It also inhibits GSK-3α/GSK-3β with IC50s of both 4 nM[3]. Alsterpaullone has antitumor activity, and is potential for the treatment of neurodegenerative and proliferative disorders. In Jurkat cell line, alsterpaullone activated caspase-9 via mitochondrial perturbation and thus induced cell apoptosis[4]. Alsterpaullone (0.5 μM) decreased Epstein-Barr virus (EBV) production in HEK293 cells by suppressing the expression of the late genes BRRF2, gB, and BKRF4[5].
作用机制	Alsterpaullone competes with ATP for binding to GSK-3α/GSK-3β.

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.41mL 0.68mL 0.34mL	17.05mL 3.41mL 1.70mL	34.10mL 6.82mL 3.41mL

参考文献

[1]Cheng W, Yang Z, Wang S, Li Y, Wei H, Tian X, Kan Q. Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures. Eur J Med Chem. 2019 Feb 15;164:615-639. doi: 10.1016/j.ejmech.2019.01.003. Epub 2019 Jan 3. PMID: 30639897. [2]Takahashi-Yanaga F. Activator or inhibitor? GSK-3 as a new drug target. Biochem Pharmacol. 2013 Jul 15;86(2):191-9. doi: 10.1016/j.bcp.2013.04.022. Epub 2013 May 2. PMID: 23643839. [3]Leost M, Schultz C, Link A, Wu YZ, Biernat J, Mandelkow EM, Bibb JA, Snyder GL, Greengard P, Zaharevitz DW, Gussio R, Senderowicz AM, Sausville EA, Kunick C, Meijer L. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem. 2000 Oct;267(19):5983-94. doi: 10.1046/j.1432-1327.2000.01673.x. PMID: 10998059. [4]Lahusen T, De Siervi A, Kunick C, Senderowicz AM. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol Carcinog. 2003 Apr;36(4):183-94. doi: 10.1002/mc.10114. PMID: 12669310. [5]Watanabe T, Sato Y, Masud HMAA, Takayama M, Matsuda H, Hara Y, Yanagi Y, Yoshida M, Goshima F, Murata T, Kimura H. Antitumor activity of cyclin-dependent kinase inhibitor alsterpaullone in Epstein-Barr virus-associated lymphoproliferative disorders. Cancer Sci. 2020 Jan;111(1):279-287. doi: 10.1111/cas.14241. Epub 2019 Dec 11. PMID: 31743514; PMCID: PMC6942432.