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Results for "

Pyruvate dehydrogenase kinase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PDHK (17) AAK1 (1) Apoptosis (3) Cannabinoid Receptor (1) CDK (1) Cyclin G-associated Kinase (GAK) (1) Drug Derivative (1) HSP (1) LIM Kinase (LIMK) (1) NKCC (1) PDK-1 (2) PROTACs (1) Reactive Oxygen Species (1) Salt-inducible Kinase (SIK) (1) Wee1 (1)
By Research Areas:	Cancer (13) Cardiovascular Disease (1) Inflammation/Immunology (6) Metabolic Disease (8)

Inhibitors & Agonists

Recombinant Proteins

Antibodies

Targets Recommended:

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-136882

TM-1	PDHK	Cancer
TM-1 is a potent inhibitor of **pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC₅₀*s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate* dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation .

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-Y0445A

Sodium dichloroacetate Maximum Cited Publications 19 Publications Verification	PDK-1 NKCC PDHK Reactive Oxygen Species Apoptosis	Cancer
Sodium dichloroacetate is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor. Sodium dichloroacetate also stimulates pyruvate dehydrogenase (PDH) activity and works as a Na ⁺-K ⁺-2Cl ⁻ cotransporter (NKCC) inhibitor. Sodium dichloroacetate prevents the phosphorylation of the E1α subunit of PDC, promoting the entry of pyruvate into the mitochondria for oxidative metabolism, reducing lactate production, and simultaneously increasing the production of reactive oxygen species (ROS). Sodium dichloroacetate inhibits tumor cell proliferation and induces apoptosis. Sodium dichloroacetate is promising for research of cancers .

HY-16082

AZD7545 2 Publications Verification	PDHK	Metabolic Disease
AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC₅₀s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively .

HY-12492

VER-246608 2 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-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-146801

PDHK-IN-3	PDHK	Metabolic Disease Cancer
PDHK-IN-3 (compound 7) is a potent PDHK (pyruvate dehydrogenase kinase) inhibitor, with IC₅₀ values of 0.21 and 1.54 μM for PDHK2 and PDHK4, respectively .

HY-162586

PDHK-IN-7	PDHK	Cancer
PDHK-IN-7 (compound 32) is an inhibitor of pyruvate dehydrogenase kinase with an IC₅₀ value of 17 nM.PDHK-IN-7 activates PDH in rat livers and has a glucose-lowering effect in Zucker fatty rats .

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-146552

PDHK-IN-4	PDHK	Metabolic Disease Cancer
PDHK-IN-4 (Compound 30) is a potent inhibitor of PDHK with IC₅₀s of 0.0051 and 0.0122 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating agent targets for numerous diseases, including diabetes and cancers. PDHK-IN-4 has the potential for the research of cancer diseases .

HY-146554

PDHK-IN-5	PDHK	Cancer
PDHK-IN-5 (Compound 19) is a potent inhibitor of PDHK with IC₅₀s of 0.006 and 0.0329 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating agent targets for numerous diseases, including diabetes and cancers. PDHK-IN-5 has the potential for the research of cancer diseases .

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-135954A

PDK4-IN-1 hydrochloride 2 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-176008

Lauric acid leelamide	Drug Derivative	Inflammation/Immunology
Lauric acid leelamide is the lauric acid (C-12) amide analog of Leelamine (HY-W005629). Leelamine exhibits inhibitory activity against pyruvate dehydrogenase kinase (PDHK) with an IC₅₀ value of 9.5 µM. Leelamine derivatives possess anti-inflammatory effects and can inhibit phospholipase A2 activity from various sources .

HY-135954

PDK4-IN-1 2 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-W005629

Leelamine	Cannabinoid Receptor PDK-1	Metabolic Disease Cancer
Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC₅₀ value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells .

HY-173298

PDHK1-IN-2	PDHK	Inflammation/Immunology Cancer
PDHK1-IN-2 (Compound 24) is an ATP-competitive dual inhibitor of pyruvate dehydrogenase kinases 1/2 (PDHK1/2), with an IC₅₀ of 0.007 μM for PDHK1 and an IC₅₀ of 0.015 μM for PDHK2. PDHK1-IN-2 can regulate immune cell metabolism and correct mitochondrial dysfunction, and is expected to be used in the research of autoimmune diseases, inflammatory diseases, cancers, and other conditions .

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 .PDK: pyruvate dehydrogenase kinase

HY-148062

RSS0680	PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1	Others
RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC with protein kinase degradation activity (Pink: FLT3-IN-17 (HY-148070); Black: Linker (HY-W041970); Blue: E3 ligase Ligand (HY-112078)). RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].

Species:	Human (2) Mouse (2)
Tag:	His (4) GST (2)
Source:	Sf9 insect cells (2) E. coli (3)

Cat. No.	Compare	Product Name	Species	Source

HY-P701737

	PDK4 Protein, Human (GST) PDK4; [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4; mitochondrial; Pyruvate dehydrogenase kinase isoform 4	Human	E. coli
	PDK4 Protein phosphorylates PDHA1 and PDHA2, inhibiting pyruvate dehydrogenase activity. This reduces glucose utilization, enhances fat metabolism, and helps maintain blood glucose levels during fasting. PDK4 also regulates fatty acid oxidation and biosynthesis, generates reactive oxygen species, protects epithelial cells, and regulates cell proliferation through metabolic regulation. PDK4 Protein, Human (GST) is the recombinant human-derived PDK4 protein, expressed by E. coli , with N-GST labeled tag.

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.

HY-P71614

	PDK3 Protein, Mouse (His) Pdk3; Pyruvate dehydrogenase kinase isoform 3	Mouse	E. coli
	PDK3 is a metabolic regulator that inhibits pyruvate dehydrogenase through PDHA1 phosphorylation to fine-tune glucose metabolism and affect aerobic respiration. Phosphorylation of PDHA2 adds another layer of control. PDK3 Protein, Mouse (His) is the recombinant mouse-derived PDK3 protein, expressed by E. coli , with N-His labeled tag.

HY-P704056

	PDK4 Protein, Mouse (221a.a, His) Pdk4; [Pyruvate dehydrogenase; acetyl-transferring)] kinase isozyme 4; mitochondrial; EC 2.7.11.2; Pyruvate dehydrogenase kinase isoform 4		E. coli
	PDK4 protein is a key kinase that regulates glucose and fatty acid metabolism by phosphorylating pyruvate dehydrogenase subunits PDHA1 and PDHA2.This inhibits pyruvate dehydrogenase activity, modulates metabolite flux and inhibits aerobic respiration.PDK4 Protein, Mouse (221a.a, His )is the recombinant mouse-derived PDK4 protein, expressed by E. coli , with N-6*His tag.

HY-P74639

	PDK4 Protein, Mouse (sf9, His-GST) Pyruvate dehydrogenase kinase isoform 4; PDK4; PDHK4	Mouse	Sf9 insect cells
	PDK4 protein is a key kinase that regulates glucose and fatty acid metabolism by phosphorylating pyruvate dehydrogenase subunits PDHA1 and PDHA2.This inhibits pyruvate dehydrogenase activity, modulates metabolite flux and inhibits aerobic respiration.PDK4 Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived PDK4 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.

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HY-P81650

	PDK2 Antibody (YA1395) PDK2; PDHK2; [Pyruvate dehydrogenase [lipoamide]] kinase isozyme 2; mitochondrial; Pyruvate dehydrogenase kinase isoform 2	WB, IHC-P, ICC/IF, IP, FC	Human, Mouse, Rat
	PDK2 Antibody (YA1395) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1395), targeting PDK2, with a predicted molecular weight of 46 kDa (observed band size: 46 kDa). PDK2 Antibody (YA1395) can be used for WB, IHC-P, ICC/IF, IP, FC experiment in human, mouse, rat background.

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