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Cat. No. Product Name CAS No. Information
PC-60606

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.

PC-60605

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.

Blood Cancer

Phase 1 Clinical

PC-42781

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.

PC-42629

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.

PC-63030

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.
PC-62481

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).
PC-62480

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.

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