PDK1 Inhibitor

OSU-03012, a derivative of the cyclooxygenase-2 (COX2) inhibitor celecoxib but lacking COX2 inhibitory activity, is a potent inhibitor of PDK1 (phosphoinositide-dependent kinase-1), a protein in the PI3K/Akt pathway that is involved in the growth and proliferation of cells [1].

OSU-03012 has been shown to induce cell death in various types of cancer cells through the inhibition of PDK1, although other mechanisms of action of this agent may be involved [2, 3]. OSU-03012-induced cell killing is dependent on protein kinase RNA-like endoplasmic reticulum kinase (PERK) [4].


Working concentration: 1-5 μM
CAS number: 742112-33-0
Synonym: 2-amino-N-(4-(5-(phenanthren-2-yl)-3-(trifluoromethyl)-1Hpyrazol-1-yl)phenyl)acetamide
Formula: C26H19F3N4O
Molecular weight: 460.45
Solubility: DMSO (10 mg/ml)
Purity: >97% (UHPLC)
Quality control:
The absence of bacterial contamination (e.g. endotoxins and peptidoglycans) is controlled using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.


10 mg OSU-03012

OSU-03012 is provided as a solid and shipped at room temperature.
Store at -20˚C. Solid product is stable 1 year at -20°C.


1. Zhu J. et al., 2004. From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res. 64(12):4309-18.
2. Yacoub A. et al., 2006. OSU-03012 promotes caspase-independent but PERK-, cathepsin B-, BID-, and AIF-dependent killing of transformed cells. Mol Pharmacol. 70(2):589-603.
3. Zhang S. et al., 2007. OSU-03012, a novel Celecoxib derivative, is cytotoxic to myeloma cells and acts through multiple mechanisms. Clin Cancer Res 13:4750-4758.
4. Park MA. et al., 2008. PERK-dependent regulation of SP70 expression and the regulation of autophagy. Autophagy. 4(3):364-7.



Description PDK1 Inhibitor
Cat. Codeinh-os03
Unit Size10 mg
Price For price or distributor address,
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