推荐产品
质量水平
检测方案
≥95% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
light yellow
溶解性
2% HCl: 10 mg/mL
2% acetic acid: 10 mg/mL
methanol: 3 mg/mL
DMSO: 4 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2
InChI key
XHBVYDAKJHETMP-UHFFFAOYSA-N
一般描述
一种细胞可透过性吡唑并嘧啶化合物，可抑制KDR/VEGFR2、ALK2/BMPR-1、AMPK激酶活性（IC50 = 25.1、148和234.6 nM），而对对ALK5/TGFβR-I、ZAPK、Syk、PKCθ、PKA或JAK3的作用却大大降低或几乎没有。研究表明，可阻断斑马鱼活体胚胎中BMP途径依赖性背腹发育（EC100 = 2.5 µ）和VEGF信号转导依赖性肌间血管形成（EC50 = 5 µM）。也可以10 mM的DMSO溶液（货号171261）提供。
生化/生理作用
主要靶标
AMPK
AMPK
产品与ATP竞争。
可逆性：是
细胞渗透性：是
阻断斑马鱼活体胚胎中BMP途径依赖性背腹发育的EC100 = 2.5 µM；阻断VEGF信号转导依赖性肌间血管形成的EC50 = 5 µM
靶标IC50：抑制KDR/VEGFR2、ALK2/BMPR-1、AMPK激酶活性分别为25.1、148和234.6 nM
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
溶解后，等分并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存至多3个月。
其他说明
Hao, J., et al. 2010.ACS Chem.Biol.5, 245.
Yu, P.B., et al. 2008. Nat. Chem. Biol4, 33.
Kim, E.K., et al. 2004.J. Biol. Chem.279, 19970.
Lee, M., et al. 2003.J. Biol. Chem.278, 39653.
Inoki, K., et al. 2003.Cell115, 577.
Fryer, L.G., 2002.FEBS Lett.531, 189.
Zhou, G., et al. 2001.J. Clin. Invest.108, 1167.
Yu, P.B., et al. 2008. Nat. Chem. Biol4, 33.
Kim, E.K., et al. 2004.J. Biol. Chem.279, 19970.
Lee, M., et al. 2003.J. Biol. Chem.278, 39653.
Inoki, K., et al. 2003.Cell115, 577.
Fryer, L.G., 2002.FEBS Lett.531, 189.
Zhou, G., et al. 2001.J. Clin. Invest.108, 1167.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
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