PDK

In the field of biochemistry, PDPK1 refers to the protein 3-phosphoinositide-dependent protein kinase-1, an enzyme which is encoded by the PDPK1 gene in humans. It is implicated in the development and progression of melanomas.PDPK1 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 PDPK1 is in the signalling pathways activated by several growth factors and hormones including insulin signaling.

Cat No.	product name
T3163	PS 48	PS 48 has been shown to be a PKB Kinase (PDK1) activator (Kd: 10.3 μM). This compound selectively binds to the PIF-binding pocket of PKB Kinase (PDK1).
T1830	BX795	BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respect...
T22350	JX06	JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.
T17224	VER-246608	VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK...
T12412L	PDK4-IN-1 hydrochloride	PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM)
T6084	Rabusertib	Rabusertib is an inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Rabusertib has been used in trials studying th...
T3895	Polyphyllin I	Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, c...
T1837	BX-912	BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC...
T24677	PS47	PS-47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1.
T2420	PHT-427	PHT-427 is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1).
T11765	KPLH1130	KPLH1130 improves glucose tolerance in HFD-fed mice. KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and att...
T0809	Dicoumarol	Dicumarol is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicumarol is a competiti...
T3604	Sodium dichloroacetate	Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to ...
T2348	GSK2334470	GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.
T2466	Osu03012	AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity...
TMA2474	δ-Tocotrienol	Delta-tocotrienol is a potential angiogenic inhibitor, it (2.5-5 microM) can significantly suppress human colorectal adenocarcinoma cells (DLD-1-CM) -induced tub...
T12566	PS10	PS10 is a ATP-competitive inhibitor of pan-PDK(PDK2, PDK4, PDK1, and PDK3 with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM , respectively).
T12398	MP7	MP7 is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).
T4046	BX517	BX-517 is a potent and selective inhibitor of PDK1.
T16450	PDK1-IN-RS2	PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-sele...
T16670	PS210	PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt, or GSK3. PS210 is a potent and selective PD...