PDK1

By Targets:	PDK-1 (17) Akt (3) Antibiotic (1) Apoptosis (3) Autophagy (3) Bacterial (1) CDK (1) EGFR (1) HIF/HIF Prolyl-Hydroxylase (2) HSP (2) IKK (2) JNK (1) Mitochondrial Metabolism (1) Monoamine Oxidase (1) mTOR (1) Parasite (1) PDHK (6) Prostaglandin Receptor (1) Pyruvate Kinase (2) Small Interfering RNA (siRNA) (3)
By Research Areas:	Cancer (24) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (2)

Targets Recommended: PDK-1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14440

MP7

PDK1 inhibitor
PDK-1 Cancer

MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.

MP7 PDK1 inhibitor	PDK-1	Cancer
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.

HY-10547

OSU-03012 4 Publications Verification AR-12; PDK1 inhibitor AR-12	PDK-1 Autophagy	Cancer
OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable *PDK-1* inhibitor with an IC₅₀ of 5 μM ^[1] .

HY-RS10273

PDK1 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
PDK1 Human Pre-designed siRNA Set A contains three designed siRNAs for PDK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

PDK1 Human Pre-designed siRNA Set A PDK1 Human Pre-designed siRNA Set A

HY-RS10274

Pdk1 Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Pdk1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pdk1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Pdk1 Mouse Pre-designed siRNA Set A Pdk1 Mouse Pre-designed siRNA Set A

HY-RS10275

Pdk1 Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Pdk1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Pdk1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Pdk1 Rat Pre-designed siRNA Set A Pdk1 Rat Pre-designed siRNA Set A

HY-114645

PDK1-IN-RS2	PDK-1	Cancer
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective *PDK1* inhibitor with a K_d of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by *PDK1* ^[1].

HY-129426

PDK1/Akt/Flt dual pathway inhibitor

Akt Cancer

PDK1/Akt/Flt dual pathway inhibitor is one of a component of KP372-1 (HY-15673 ), and inhibits PDK1/Akt/Flt dual pathway ^[1].

PDK1/Akt/Flt dual pathway inhibitor	Akt	Cancer
PDK1/Akt/Flt dual pathway inhibitor is one of a component of KP372-1 (HY-15673 ), and inhibits PDK1/Akt/Flt dual pathway ^[1].

HY-149275

*PKM2/PDK1-IN-1*	Pyruvate Kinase PDK-1 Akt EGFR Apoptosis	Cancer
PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of *PKM2/PDK1*. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway ^[1].

HY-13856

(R)-PS210	PDK-1	Cancer
(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of *PDK1* with an AC₅₀ value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment ^[1].

HY-121629

PS210	PDK-1	Cancer
PS210 is a potent and selective *PDK1* activator with a K_d of 3 μM and targets the PIF-binding pocket of *PDK1. PS210 is inactive against other protein kinases, including PDK1* downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of *PDK1*, inhibiting the phosphorylation and activation of S6K ^[1] .

HY-10515

BX-320	PDK-1	Cancer
BX-320 is a selective, ATP-competitive, orally acitive, and direct *PDK1* inhibitor with an IC₅₀ of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect ^[1].

HY-11005

BX-912 4 Publications Verification	PDK-1 Apoptosis	Cancer
BX-912 is a direct, selective, and ATP-competitive *PDK1* inhibitor (IC₅₀=26 nM). BX-912 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 ^[1].

HY-13842

BX517

1 Publications Verification

PDK-1 Cancer

BX517 is a potent and selective inhibitor of PDK1 with IC₅₀ of 6 nM.
HY-15967

PS48

5 Publications Verification

PDK-1 Cancer

PS48 is an activator of PDK1 with an AC₅₀ of 8 μM.
HY-14981

GSK2334470

5+ Cited Publications

PDK-1 Cancer

GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC₅₀ of 10 nM.
HY-P5450

PDKtide

PDK-1 Others

PDKtide is a biological active peptide. (This peptide is a substrate for PDK1 (Phosphatidylinositide-Dependent Kinase 1).)

BX517 1 Publications Verification	PDK-1	Cancer
BX517 is a potent and selective inhibitor of *PDK1* with IC₅₀ of 6 nM.

PS48 5 Publications Verification	PDK-1	Cancer
PS48 is an activator of *PDK1* with an AC₅₀ of 8 μM.

GSK2334470 5+ Cited Publications	PDK-1	Cancer
GSK2334470 is a highly specific and potent inhibitor of *PDK1* with an IC₅₀ of 10 nM.

PDKtide	PDK-1	Others
PDKtide is a biological active peptide. (This peptide is a substrate for PDK1 (Phosphatidylinositide-Dependent Kinase 1).)

HY-151465

HIF-1α-IN-4	HIF/HIF Prolyl-Hydroxylase	Cancer
HIF-1α-IN-4 is a *HIF-1α* inhibitor with an IC₅₀ value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer ^[1].

HY-19564

JX06 1 Publications Verification
JX06 is a potent, selective and covalent inhibitor of *PDK. JX06 inhibits PDK1, PDK2* and *PDK3* with IC₅₀s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity ^[1].

HY-135773

CRTh2 antagonist 3	Prostaglandin Receptor PDK-1	Cardiovascular Disease Inflammation/Immunology
CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist ^[1]. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC₅₀ of 2 μM and a K_d of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation .

HY-12492

VER-246608 1 Publications Verification	PDHK	Cancer
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC₅₀s of 35 nM, 40 nM, 84 nM, and 91 nM for *PDK-1, PDK-3, PDK-2, and PDK-4*, respectively.

HY-151466

HIF-1α-IN-5	HIF/HIF Prolyl-Hydroxylase Monoamine Oxidase	Cancer
HIF-1α-IN-5 is a *HIF-1α* inhibitor with an IC₅₀ value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer ^[1].

HY-N0645

Dicoumarol 5+ Cited Publications Dicumarol	PDHK	Cancer
Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and *PDK1* with IC₅₀s of 0.37 and 19.42 μM, respectively.

HY-13851

PS47

PDK-1 Others

PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48 ^[1] .

PS47	PDK-1	Others
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48 ^[1] .

HY-15569

NU6102	CDK	Cancer
NU6102 is a potent *CDK1* and CDK2 inhibitor with IC₅₀s of 9.5 nM and 5.4 nM for *CDK1/cyclinB* and CDK2/cyclinA3, respectively. NU6102 shows selectivity for *CDK1/CDK2* over CDK4 (IC₅₀ of 1.6 μM), DYRK1A (IC₅₀ of 0.9 μM), PDK1 (IC₅₀ of 0.8 μM) and ROCKII (IC₅₀ of 0.6 μM) ^[1] .

HY-N0047

Polyphyllin I 1 Publications Verification	JNK mTOR Akt PDK-1 Autophagy Apoptosis	Cancer
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of *PDK1/Akt/mTOR* signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis ^[1] .

HY-149814

PDK-IN-1	PDHK HSP	Cancer
PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC₅₀ values of 0.03 and 0.1 μM for *PDK1* and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass ^[1].

HY-156109

PDK-IN-2	PDHK Mitochondrial Metabolism	Cancer
PDK-IN-2 (Compound 1F) is a *PDK* inhibitor (IC₅₀: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model ^[1].

HY-N6769

Radicicol 3 Publications Verification Monorden	HSP Bacterial Antibiotic Parasite	Infection
Radicicol is an inhibitor of Hsp90 with an IC₅₀ value < 1 μM, and leads to proteasomal degradation ^[1]. Radicicol exhibits inhibition on *PDK* with IC₅₀s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC₅₀ value of 16.04 μM .

HY-10514

BX795 Maximum Cited Publications 22 Publications Verification	PDK-1 IKK Autophagy	Cancer
BX795 is a potent and selective inhibitor of *PDK1, with an IC₅₀* of 6 nM. BX795 is also a potent and relatively specific inhibitor of *TBK1* and IKKε, with an IC₅₀ of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy ^[1] .

HY-124652

TBK1/IKKε-IN-4	IKK	Cancer
TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective *TBK1* and IKKε inhibitor with IC₅₀ values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR ^[1].

HY-156375

PKM2 activator 6	Pyruvate Kinase PDK-1	Cancer
PKM2 activator 6 (Compound Z10) is a PKM2 activator and *PDK1* inhibitor (K_D: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC₅₀: 10.04, 2.16, 3.57, 66.39 μM) ^[1].

HY-121744

PS10 2 Publications Verification	PDHK	Inflammation/Immunology
PS10 is a novel, potent and ATP-competitive pan-PDK* inhibitor,* inhibits all PDK isoforms with IC₅₀ of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (K_d= 239 nM) than for Hsp90 (K_d= 47 μM) ^[1]. PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy ^[2].PDK: pyruvate dehydrogenase kinase

HY-157299

PDK-IN-3	PDHK	Cancer
PDK-IN-3 (compound 1) is a potent pan inhibitor of *PDK* with IC₅₀s of 109.3, 135.8, 458.7 nM and 8.67 μM against PDK 1-4, respectively. PDK-IN-3 also induces proliferation and apoptosis in A549 cells ^[1].

Cat. No.	Product Name

HY-L015

PI3K/Akt/mTOR Compound Library	568 compounds
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials. MCE owns a unique collection of 568 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

PI3K/Akt/mTOR Compound Library

568 compounds

The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.

MCE owns a unique collection of 568 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

Cat. No.	Product Name	Target	Research Area

HY-P5450

PDKtide

PDK-1 Others

PDKtide is a biological active peptide. (This peptide is a substrate for PDK1 (Phosphatidylinositide-Dependent Kinase 1).)

PDKtide	PDK-1	Others
PDKtide is a biological active peptide. (This peptide is a substrate for PDK1 (Phosphatidylinositide-Dependent Kinase 1).)

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0645

Dicoumarol Maximum Cited Publications 8 Publications Verification Dicumarol	Structural Classification Melilotus officinalis (L.) Pall. Classification of Application Fields Leguminosae Source classification Coumarins Phenylpropanoids Plants Disease Research Fields Biological Pesticide Research Cancer Agricultural Research	PDHK
Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and *PDK1* with IC₅₀s of 0.37 and 19.42 μM, respectively.

HY-N0047

Polyphyllin I 1 Publications Verification	Structural Classification Liliaceae Classification of Application Fields Paris polyphylla Smith Plants Disease Research Fields Saccharides Steroids Cancer	JNK mTOR Akt PDK-1 Autophagy Apoptosis
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of *PDK1/Akt/mTOR* signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis ^[1] .

HY-N6769

Radicicol 3 Publications Verification Monorden	Structural Classification Antifungal Classification of Application Fields Source classification Marine natural products Anti-parasitic Disease Research Infection Microorganisms Macrolide Antibiotics Antibiotics Phenols Polyphenols Disease Research Fields Marine microorganism	HSP Bacterial Antibiotic Parasite
Radicicol is an inhibitor of Hsp90 with an IC₅₀ value < 1 μM, and leads to proteasomal degradation ^[1]. Radicicol exhibits inhibition on *PDK* with IC₅₀s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC₅₀ value of 16.04 μM .

Cat. No.	Compare	Product Name	Species	Source

HY-P73718

	PDK1 Protein, Human (sf9, His) Pyruvate dehydrogenase kinase isoform 1; PDK1; PDHK1	Human	Sf9 insect cells
	PDK1 protein is a key kinase that controls glucose and fatty acid metabolism by phosphorylating pyruvate dehydrogenase subunits PDHA1 and PDHA2. This molecular switch inhibits pyruvate dehydrogenase, fine-tunes metabolite flux and downregulates aerobic respiration. PDK1 Protein, Human (sf9, His) is the recombinant human-derived PDK1 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of PDK1 Protein, Human (sf9, His) is 408 a.a., with molecular weight of ~45 kDa.


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Cat. No.	Product Name	Application	Reactivity

HY-P80272

PDK1 Antibody	WB, IHC-P, IP, FC	Human, Mouse, Rat
PDK1 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 49 kDa, targeting to PDK1. It can be used for WB,IHC-P,IP,FC assays with tag free, in the background of Human, Mouse, Rat.

HY-P81824

PDPK1 Antibody (YA1569)

PDPK1; PDK1; 3-phosphoinositide-dependent protein kinase 1; hPDK1
WB Human, Mouse, Rat

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