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
InChI key
DFURSNCTQGJRRX-JYRVWZFOSA-N
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-
assay
≥95% (sum of two isomers, HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
dark brown
solubility
DMSO: 25 mg/mL
shipped in
ambient
Quality Level
General description
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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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