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.
Synonym(s):
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
Empirical Formula (Hill Notation):
C15H14N4O2
CAS Number:
Molecular Weight:
282.30
UNSPSC Code:
12352200
Assay:
≥95% (sum of two isomers, HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
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
storage temp.
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
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)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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