BX-795, BX-912, and BX-320: potent PDK1 inhibitors with IC50 = 11-30 nM
     
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BX-795, BX-912, and BX-320: potent PDK1 inhibitors with IC50 = 11-30 nM

N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide (BX-795)

BX-795
OTAVAchemicals Catalogue Number: 7070707044
CAS Registry Number: 702675-74-9
Purity: 95%+ (HPLC)

N-[3-[[5-Bromo-4-[[2-(1H-imidazol-4-yl)ethyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide (BX-912)

BX-912
OTAVAchemicals Catalogue Number: 7070707060
CAS Registry Number: 702674-56-4
Purity: 95%+ (HPLC)

N1-[3-[[5-Bromo-2-[[3-[(1-pyrrolidinylcarbonyl)amino]phenyl]amino]-4-pyrimidinyl]amino]propyl]-2,2-dimethylpropanediamide (BX-320)

BX-320
OTAVAchemicals Catalogue Number: 7070707045
CAS Registry Number: 702676-93-5
Purity: 95%+ (HPLC)


Ref.: Feldman et al. Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1. Journal of Biological Chemistry (2005), 280, 19867-19874


Abstract: The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs. Here, we describe three potent PDK1 inhibitors, BX-795, BX-912, and BX-320 (IC50 = 1130 nM) and their initial biological characterization. The inhibitors blocked PDK1/Akt signaling in tumor cells and inhibited the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis. A number of cancer cell lines with elevated Akt activity were >30-fold more sensitive to growth inhibition by PDK1 inhibitors in soft agar than on tissue culture plastic, consistent with the cell survival function of the PDK1/Akt signaling pathway, which is particularly important for unattached cells. BX-320 inhibited the growth of LOX melanoma tumors in the lungs of nude mice after injection of tumor cells into the tail vein. The effect of BX-320 on cancer cell growth in vitro and in vivo indicates that PDK1 inhibitors may have clinical utility as anticancer agents.

 
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