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Search Results for " pyruvate dehydrogenase kinase "

Targets Recommended: Dehydrogenase PDK

14

抑制剂 & 化合物

2

天然产物

5

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T11765	KPLH1130	Dehydrogenase; PDK	Metabolism; PI3K/Akt/mTOR signaling
	KPLH1130，一种选择性丙酮酸脱氢酶激酶(PDK)抑制剂，在高脂饮食(HFD)喂养的小鼠中提高了糖耐量。KPLH1130 抑制巨噬细胞极化并减轻了炎症反应。
T2447	AZD7545	Dehydrogenase	Metabolism
	AZD7545 是竞争性和选择性的PDHK2抑制剂，能够抑制PDHK1和PDHK2的活性，其IC50值分别为 36.8 nM 和 6.4 nM。
T22350	JX06	Apoptosis; Dehydrogenase; PDK	Apoptosis; Metabolism; PI3K/Akt/mTOR signaling
	JX06 是一种选择性共价PDK 抑制剂，抑制PDK1,PDK2和PDK3，IC50值分别为 49 nM，101 nM 和 313 nM。它以不可逆的方式与半胱氨酸残基共价结合来抑制PDK1活性，具有抗肿瘤活性。
T17224	VER-246608	Dehydrogenase; PDK	Metabolism; PI3K/Akt/mTOR signaling
	VER-246608 是ATP 竞争性的丙酮酸脱氢酶激酶抑制剂，对PDK-1，PDK-3，PDK-2，和PDK-4的IC50分别为 35 nM，40 nM，84 nM 和 91 nM。
T12412L	PDK4-IN-1 hydrochloride	Apoptosis; PDK	Apoptosis; PI3K/Akt/mTOR signaling
	PDK4-IN-1 hydrochloride 是一种蒽醌衍生物，对丙酮酸脱氢酶激酶 4有抑制作用，IC50为 84 nM，具有口服活性。它抑制细胞转化和细胞增殖并诱导细胞凋亡。它具有抗过敏，抗糖尿病和抗癌作用。
T19783	Dehydroabiethylamine NSC-2955,NSC 2955,Dehydroabietylamine,NSC2955,Leelamine free base,Leelamine,脱氢松香胺	P450; PDK	Metabolism; PI3K/Akt/mTOR signaling
	Dehydroabiethylamine (NSC-2955) 是肝脏 CYP2B 活性的诱导剂。 Dehydroabiethylamine 抑制丙酮酸脱氢酶激酶 (PDK) 和细胞内胆固醇转运，具有抗肿瘤活性。
T15944	M77976	PDK	PI3K/Akt/mTOR signaling
	M77976 是一种选择性 ATP 竞争丙酮酸脱氢酶激酶 PDK4 抑制剂，对 PDK4 有抑制作用，IC50 值为 648 μM。M77976 有用于研究肥胖症和糖尿病。
T15362	FX-11 LDHA Inhibitor FX11	Dehydrogenase	Metabolism
	FX-11 (LDHA Inhibitor FX11) 是一种有效的、选择性的和竞争性的乳酸脱氢酶 A (LDHA) 的特异性抑制剂，对LDHA 的Ki 为 8 μM。FX-11 对PKM2 (丙酮酸激酶 M2)具有激活作用。FX-11 可降低 ATP 水平，诱导氧化应激和ROS 生成，可引起细胞死亡。FX-11 在淋巴瘤和胰腺癌异种移植过程中表现出抗肿瘤活性。
T12412	PDK4-IN-1	Others	Others
	PDK4-IN-1 is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM).
T63012	TM-1	Others	Others
	TM-1 是一种强效的丙酮酸脱氢酶激酶 (PDHK) 抑制剂，能够抑制 PDHK1 (IC50: 2.97 μM) 和 PDHK2 (IC50: 5.2 μM)的活性。TM-1 可以阻断丙酮酸脱氢酶复合物 (PDHC) 磷酸化，并抑制癌细胞增殖。
T60527	PDHK-IN-3	Others	Others
	PDHK-IN-3 (compound 7) 是有效的丙酮酸脱氢酶激酶(PDHK)抑制剂，对PDHK2的IC50值为0.21μM，对PDHK4的IC50值为1.54 μM。
T74830	PDK-IN-1	Others	Others
	PDK-IN-1（compound 7o）是一种针对丙酮酸脱氢酶激酶（PDK）的抑制剂，其对PDK1和HSP90的IC50值分别为0.03和0.1μM。通过靶向PDH/PDK轴，PDK-IN-1能有效降低肿瘤质量。
T81788	Mito-SilylDCA	Others	Others
	Mito-SilylDCA 是一种针对线粒体网络中的 PDK1 的丙酮酸氢酶激酶抑制剂。这种化合物结合了具有靶向 TPP 部分的 DCA 分子，以及聚乙烯长链与硅基，以实现其对 PDK1 的抑制作用。
T37355	CAY10703	Others	Others
	Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against perip...

化合物

Cat.No: T11765

Target: Dehydrogenase, PDK

Cat.No: T2447

Target: Dehydrogenase

Cat.No: T22350

Target: Apoptosis, Dehydrogenase, PDK

Cat.No: T17224

Target: Dehydrogenase, PDK

PDK4-IN-1 hydrochloride

Cat.No: T12412L

Target: Apoptosis, PDK

Dehydroabiethylamine

Cat.No: T19783

Synonym: NSC-2955,NSC 2955,Dehydroabietylamine,NSC2955,Leelamine free base,Leelamine,脱氢松香胺

Target: P450, PDK

Cat.No: T15944

Target: PDK

Cat.No: T15362

Synonym: LDHA Inhibitor FX11

Target: Dehydrogenase

Cat.No: T12412

Target: Others

Cat.No: T63012

Target: Others

Cat.No: T60527

Target: Others

Cat.No: T74830

Target: Others

Cat.No: T81788

Target: Others

Cat.No: T37355

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T0809	Dicoumarol Dicumarol,双羟香豆素,双香豆素	Dehydrogenase; NADPH; PDK	Metabolism; PI3K/Akt/mTOR signaling
	Dicoumarol (Dicumarol) 是一种 NAD(P)H: 醌氧化还原酶 1 和PDK1的抑制剂，它们的IC50值分别为 0.37 和 19.42 μM。
T3604	Sodium dichloroacetate Sodium Dichloroacetate,DCA,bichloroacetic acid,二氯乙酸钠,Sodium dichloroacetate (DCA),二氯醋酸酯	Apoptosis; Dehydrogenase; Reactive Oxygen Species; PDK	Apoptosis; Immunology/Inflammation; Metabolism; NF-κB; PI3K/Akt/mTOR signaling
	Sodium dichloroacetate (DCA) 是一种肿瘤细胞线粒体中的代谢调节剂，一种丙酮酸脱氢酶激酶 (PDK) 抑制剂。Sodium dichloroacetate 具有抗肿瘤活性，可以降低肿瘤微环境中的乳酸，增加活性氧的产生并促进肿瘤细胞凋亡。

天然产物

Cat.No: T0809

Synonym: Dicumarol,双羟香豆素,双香豆素

Target: Dehydrogenase, NADPH, PDK

Sodium dichloroacetate

Cat.No: T3604

Synonym: Sodium Dichloroacetate,DCA,bichloroacetic acid,二氯乙酸钠,Sodium dichloroacetate (DCA),二氯醋酸酯

Target: Apoptosis, Dehydrogenase, Reactive Oxygen Species, PDK

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-04568	PDK1 Protein, Human, Recombinant (His) pyruvate dehydrogenase kinase, is...	Human	Baculovirus Insect Cells
	Pyruvate dehydrogenase kinase, isozyme 1, also known as [Pyruvate dehydrogenase [lipoamide]] kinase isozyme 1, mitochondrial and PDK1, is a member of the PDK / BCKDK protein kinase family. PDK-1 is expressed predominantly in the heart. It contains one histidine kinase domain. Pyruvate dehydrogenase kinase (PDK) isoforms are molecular switches that downregulate the pyruvate dehydrogenase complex (PDC) by reversible phosphorylation in mitochondria. An inhibitory effect of lipoic acid on PDKs would...
TMPY-04445	PDK4 Protein, Mouse, Recombinant (His & GST) AV005916,pyruvate dehydrogenase kinase...	Mouse	Baculovirus Insect Cells
	Pyruvate dehydrogenase kinase 4 (PDK4) is a mitochondrial protein that regulates the TCA cycle.PDK4, a vital mitochondrial protein, controls the switch between glycolysis and oxidative phosphorylation based upon nutrient availability.Pyruvate dehydrogenase kinase 4 (PDK4) mRNA has been reported as an up-regulated gene in the heart and skeletal muscle of carnitine-deficient juvenile visceral steatosis (JVS) mice under fed conditions. PDK4 plays an important role in the inhibition of glucose oxida...
TMPH-02469	PDK1 Protein, Mouse, Recombinant (His) Pdk1,Pyruvate dehydrogenase kinase	Mouse	Baculovirus Insect Cells
	PDK1 Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with N-10xHis tag. The predicted molecular weight is 48.7 kDa and the accession number is Q8BFP9.
TMPH-02470	PDK3 Protein, Mouse, Recombinant (His) Pdk3,[Pyruvate dehydrogenase (acetyl-trans...	Mouse	E. coli
	PDK3 Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 30.3 kDa and the accession number is Q922H2.
TMPJ-00955	MDH1 Protein, Human, Recombinant (His) Cytosolic Malate Dehydrogenase,MDH1,MDHA,Diiodophen...	Human	E. coli
	Malate Dehydrogenase, Cytoplasmic (MDH1) is an enzyme which belongs to the MDH Type 2 sub-family of LDH/MDH superfamily. MDH1 is involved in the Citric Acid Cycle that catalyzes the conversion of Malate into Oxaloacetate (using NAD+) and vice versa. MDH1 should not be confused with Malic Enzyme, which catalyzes the conversion of Malate to Pyruvate, producing NADPH. MDH1 also participates in Gluconeogenesis, the synthesis of Glucose from smaller molecules. Pyruvate in the mitochondria is acted up...

重组蛋白

PDK1 Protein, Human, Recombinant (His)

Cat.No: TMPY-04568

Species: Human

Expression System: Baculovirus Insect Cells

PDK4 Protein, Mouse, Recombinant (His & GST)

Cat.No: TMPY-04445

Species: Mouse

Expression System: Baculovirus Insect Cells

PDK1 Protein, Mouse, Recombinant (His)

Cat.No: TMPH-02469

Species: Mouse

Expression System: Baculovirus Insect Cells

PDK3 Protein, Mouse, Recombinant (His)

Cat.No: TMPH-02470

Species: Mouse

Expression System: E. coli

MDH1 Protein, Human, Recombinant (His)

Cat.No: TMPJ-00955

Species: Human

Expression System: E. coli

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