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521276

PDK1 Inhibitor II

Name: PDK1 Inhibitor II
Brand: MM

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:

850717-64-5

Molecular Weight:

282.30

UNSPSC Code:

12352200

Assay:

≥95% (sum of two isomers, HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Quality Level

100

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.

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