PDK1 Selective Inhibitors | Activators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S1274 BX-795

BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1.

Selective PDK-1, IC50: 6 nM
S7087 GSK2334470

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

Selective PDK-1, IC50: 10 nM
S1106 OSU-03012 (AR-12)

OSU-03012 (AR-12) is a potent inhibitor of recombinant PDK-1(phosphoinositide-dependent kinase 1) with IC50 of 5 μM in a cell-free assay and 2-fold increase in potency over OSU-02067.

Selective PDK-1, IC50: 5 μM
S1556 PHT-427

PHT-427 (CS-0223) is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.

Selective PDK1, Ki: 5.2 μM
S2272 Indoprofen

Indoprofen is a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor. Indoprofen prevents muscle wasting in aged mice through activation of PDK1/AKT pathway.Indoprofen selectively increases SMN2-luciferase reporter protein and endogenous SMN protein.

S7586 PS-48

PS-48 is an allosteric activator of phosphoinositide-dependent protein kinase-1 (PDK1).

S0983 JX06

JX06 as a selective covalent inhibitor of PDK1 in cells. JX06 dose-dependently inhibits PDK1, PDK2 and PDK3 with IC50 0.049 μM, 0.101 μM and 0.313 μM, respectively.

Pan PDK1, IC50: 0.049 μM