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PDK Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PDK-1 (14) Akt (3) Antibiotic (1) Apoptosis (5) Autophagy (3) Bacterial (1) Cannabinoid Receptor (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 (12) Pyruvate Kinase (2)
By Research Areas:	Cancer (27) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (4) Metabolic Disease (4)

Inhibitors & Agonists

Screening Libraries

Natural
Products

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 .

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-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 .

**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 .

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 .

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 .

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 .

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* .

HY-135954A

PDK4-IN-1 hydrochloride 1 Publications Verification	PDHK Apoptosis	Metabolic Disease Inflammation/Immunology Cancer
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC₅₀ value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity .

HY-135954

PDK4-IN-1 1 Publications Verification	PDHK Apoptosis	Metabolic Disease Inflammation/Immunology Cancer
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC₅₀ value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity .

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 .

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 .

HY-157538

PDK4-IN-2	PDHK	Cardiovascular Disease
PDK4-IN-2 (compound 8) is a pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC₅₀ of 46 µM. PDK4-IN-2 improves ejection fraction of failing hearts by regulating bioenergetics via activation of the tricarboxylic acid cycle .

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) . 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-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 .

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 .

HY-146977

LDHA/PDKs-IN-1	PDK-1	Cancer
LDHA/PDKs-IN-1 (compound 20e) is a potent and dual inhibitor of PDKs and LDHA with IC₅₀s of 0.8 and 0.15 μM, respectively. LDHA/PDKs-IN-1 reduces A549 cell proliferation with an EC₅₀ of 13.2 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-1 has the potential for the research of cancer diseases .

HY-146978

LDHA/PDKs-IN-2	PDK-1	Cancer
LDHA/PDKs-IN-2 (compound 20k) is a potent and dual inhibitor of PDKs and LDHA with IC₅₀s of 1.6 and 0.7 μM, respectively. LDHA/PDKs-IN-2 reduces A549 cell proliferation with an EC₅₀ of 15.7 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-2 has the potential for the research of cancer diseases .

HY-13842

BX517

1 Publications Verification

PDK-1 Cancer

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

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

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

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 . 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-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 .

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-W005629

Leelamine	Cannabinoid Receptor PDHK	Cancer
Leelamine is a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine also inhibits pyruvate dehydrogenase kinases (PDKs). Leelamine exhibits anti-tumor activity .

HY-128578

KPLH1130	PDHK	Metabolic Disease Inflammation/Immunology
KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice .

HY-114702

M77976 1 Publications Verification	PDHK	Metabolic Disease
M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC₅₀ of 648 μM. M77976 is potential for the research of obesity and diabetes .

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 .

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 .

HY-10514

BX795 Maximum Cited Publications 23 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 .

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 .

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) .

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 .

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) .

PI3K/Akt/mTOR Compound Library	575 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 575 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.

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 . 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 .

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 .

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.

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PDK Inhibitor

Inhibitors & Agonists

Screening Libraries

NaturalProducts

Natural
Products