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You are here:Home-Inhibitors & Agonists-PI3K/Akt/mTOR Pathway-PDK1

Request The Product List ofPDK1 PDK1

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
H6993

PDK1 inhibitor 7

 		1001409-50-2

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).
H6992

OSU-03013

 		742112-34-1

OSU-03013 (OSU 03013, OSU03013) is a novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 2 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.
H6991

OSU-03012

 		742112-33-0

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.
H6990

BX795

 		702675-74-9

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.
H6989

BX-912

 		702674-56-4

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.
H6988

BX-320

 		702676-93-5

BX-320 is a potent, selective and ATP-competitive inhibitor of PDK1 with IC50 of 30 nM, >20-fold selectivity over PKA; 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; inhibits the growth of LOX melanoma tumors in the lungs of nude mice.
H6995

PS 423

 		1221964-37-9

PS 423 is a substrate-selective inhibitor of PDK1, inhibits the phosphorylation and activation of S6K without affecting the PKB/Akt signaling pathway in HEK293 cells, the prodrug of PS210; inhibits glucose uptake in C2C12 myoblasts; inhibits S6K but not PKB/Akt downstream signaling in muscle cells.
H6994

PS 210

 		1221962-86-2

PS 210 is a potent, specific activator of PDK1 that target the PIF-binding pocket of PDK1, does not alter the activity of any of the 121 kinases (S6K, PKB/Akt or GSK3).

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