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

potent PDK1 inhibitors IC50 = 6 nM

Chemical Formula: C20H23BrN8O

Molecular Weight: 471.4

OTAVAchemicals Catalogue Number: 7070707060

CAS Registry Number: 304896-28-4

Purity: 97% (HPLC)

2-Amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-acetamide (OSU03012)

• OSU03012 has an IC50 of 5 µM for inhibition of 3-phosphoinositide-dependent kinase-1 (PDK-1), and therefore Akt activation, with no measurable COX-2 inhibition up to 50 µM. OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 µM across a panel of 60 cancer cell lines. It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway. OSU03012 induces apoptosis of chronic lymphocytic leukemia (CLL) cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways

OTAVAchemicals Catalogue Number: 7070707053

CAS Registry Number: 742112-33-0

Purity: 95%+ (HPLC)

Chemical Formula: C23H31BrN8O3

Molecular Weight: 547.5

OTAVAchemicals Catalogue Number: 7070707045

CAS Registry Number: 702676-93-5

Purity: 90%+ (HPLC)

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

potent PDK1 inhibitors IC50 = 30 nM

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

highlighted BX 795 bioactivitiy as a potent and relatively specific inhibitor of TBK1 and closely related IKKe, with IC50 values to be 6, 41, and 111 nM for TBK1, IKKe and PDK1 respectively

OTAVAchemicals Catalogue Number: 7070707044

CAS Registry Number: 702675-74-9

Purity: 95%+ (HPLC)