Signaling Pathway

PDK-1

PDK-1

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PDK1 (3-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. PDK1 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 PDK1 is in the signalling pathways activated by several growth factors and hormones including insulin signaling. More recent data indicate that alteration of PDK1 is a critical component of oncogenic PI3K signalling in breast cancer, suggesting that inhibition of PDK1 can inhibit breast cancer progression. PDK1 has an essential role in regulating cell migration especially in the context of PDK1 deficiency. PDK1 is a valid therapeutic target and suggests that PDK1 inhibitors may be useful to prevent cancer progression and abnormal tissue dissemination.

PDK-1 Inhibitors & Modulators (7)

Product Name Catalog No. Brief Description
BX-912

HY-11005

BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM; >10 fold selectivity over PKA, PKC, C-Kit, EGFR etc.

BX517

HY-13842

BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.

BX795

HY-10514

BX795 is a potent and selective dual inhibitor of TBK1/PDK1 with IC50s of 2 nM/6 nM respectively; > 50 fold selectivity over PKA, PKC, c-Kit, GSK3β etc.

GSK2334470

HY-14981

GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM, with no activity at other close related AGC-kinases.

NVP-BAG956

HY-13333

NVP-BAG956(BAG 956) is a potent, ATP-competitive and selective dual PI3K and PDK1 inhibitor in vitro and in vivo,with IC50 values to be 56, 444, 34, 117 and 240 nM for PI3K p110 alpha, beta, delta and gamma and PDK1 kinases, respectively.

PDK1 inhibitor

HY-14440

PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent.

TEPP-46

HY-18657

TEPP-46 is a potent and selective activator of recombinant pyruvate kinase M2 (PKM2) with half-maximum activating concentration (AC50 value) of 92 nM, and little or no activity versus PKM1, PKL and PKR.