PDK-1 (phosphoinositide dependent protein kinase-1) is a protein which in humans is encoded by the PDK1 gene. It is implicated in the development and progression of melanomas. PDK-1 is a master kinase, which is crucial for the activation of AKT/PKB and many other AGC kinases including PKC, S6K, SGK. An important role for PDK-1 is in the signalling pathways activated by several growth factors and hormones including insulin signaling. More recent data indicate that alteration of PDK-1 is a critical component of oncogenic PI3K signalling in breast cancer, suggesting that inhibition of PDK-1 can inhibit breast cancer progression. PDK-1 has an essential role in regulating cell migration especially in the context of PDK-1 deficiency. PDK-1 is a valid therapeutic target and suggests that PDK-1 inhibitors may be useful to prevent cancer progression and abnormal tissue dissemination.
|Cat. No.||Product Name||CAS No.||Information|
PDK1 inhibitor 7
A potent, selective PDK1 inhibitor with IC50 of 1 nM, displays >3,000-fold selectivity against a panel of 256 kinases; specifically inhibits cellular PDK1 T-loop phosphorylation (Ser-241), inhibits p-RSK S221 in PC-3 cells with EC50 of 300 nM, inhibits colony formation in a subset of cancer cell lines (4 of 10) and primary xenograft tumor lines (9 of 57).
BX-912 (BX912) is a potent, selective and ATP-competitive inhibitor of PDK1 with IC50 of 26 nM; blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
OSU-03012 (AR-12) is a novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 5 uM; induces apoptosis in PC-3 cells at low microM range, causes Akt dephosphorylation and inhibition of p70 S6 kinase activity; displays cytotocixity against a panel of 60 cell lines with mean GI50 of 3 uM; decreases incidences of carcinoma and metastasis in transgenic mouse model of prostate cancer.
BX795 is a potent and relatively specific PDK1 inhibitor with IC50 of 6 nM; also inhibits TBK1 and IKKε with IC50 of 6 nM and 41 nM; shows no activity for PKA, PKC, c-Kit, GSK3β, IKKα, IKKβ, etc.; blocks the autophosphorylation of overexpressed TBK1 and IKKepsilon at Ser-172; has no effect on the canonical NFkappaB signaling pathway.
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