521276
PDK1 Inhibitor II
The PDK1 Inhibitor II, also referenced under CAS 850717-64-5, controls the biological activity of PDK1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
PDK1 Inhibitor II, 2-Oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]indolin-5-yl]urea, BX-517
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About This Item
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质量水平
方案
≥95% (sum of two isomers, HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
dark brown
溶解性
DMSO: 25 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C15H14N4O2/c1-8(11-3-2-6-17-11)13-10-7-9(18-15(16)21)4-5-12(10)19-14(13)20/h2-7,17H,1H3,(H,19,20)(H3,16,18,21)/b13-8-
InChI key
DFURSNCTQGJRRX-JYRVWZFOSA-N
一般描述
A cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDK1 inhibitor (IC50 = 6 nM) and effectively suppresses cellular Akt Thr308 phosphorylation level in PC-3 cultures (IC50 ≤1 µM), while affecting PKA (IC50 = 1.6 µM) and 7 other kinases (IC50 ≥600 nM) only at much higher concentrations. Its in vivo applicability is limited by a low aqueous solubility (2 µg/ml in PBS) and poor pharmacokinetics.
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Islam, I., et al. 2007. Bioorg. Med. Chem. Lett.17, 3819.
Islam, I., et al. 2007. Bioorg. Med. Chem. Lett.17, 3814.
Islam, I., et al. 2007. Bioorg. Med. Chem. Lett.17, 3814.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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