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Search Results for " PDK "

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阻害剤

天然化合物

リコンビナントタンパク質

カタログ番号	製品名	別名	ターゲット
T79723	PDK-IN-2
	PDK-IN-2 (Compound 1F), with an IC50 of 68 nM, is a potent PDK inhibitor that downregulates the expression of PDK1 and PDK4 in cells. It promotes mitochondrial bioenergetics, reduces glycolytic activity, and triggers apo...
T74830	PDK-IN-1
	PDK-IN-1 (compound 7o), a pyruvate dehydrogenase kinase (PDK) inhibitor, exhibits IC50 values of 0.03 and 0.1 μM against PDK1 and HSP90, respectively. This compound effectively targets the PDH/PDK axis, significantly red...
T2348	GSK2334470		PDK
	GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.		PDK
T1837	BX-912		Apoptosis , VEGFR , PKA , Chk , CDK , PDK
	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 etc.		Apoptosis , VEGFR , PKA , Chk , CDK , PDK
T1830	BX795		IκB/IKK , Chk , CDK , c-Kit , PDK , Autophagy
	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, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than...		IκB/IKK , Chk , CDK , c-Kit , PDK , Autophagy
T24677	PS47	PS 47,PS-47	PDK
	PS-47(PS 47) is an inactive E-isomer of PS48. PS48 is an activator of PDK1.		PDK
T4046	BX517	PDK1 inhibitor 2,BX 517,BX-517	Akt , PDK
	BX517 (PDK1 inhibitor 2) is a potent and selective inhibitor of PDK1.		Akt , PDK
T16670	PS210		PDK
	PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1, without acting against other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves ...		PDK
T12398	MP7	PDK1 inhibitor	PDK
			PDK
T12412L	PDK4-IN-1 hydrochloride		Apoptosis , PDK
			Apoptosis , PDK
T12412	PDK4-IN-1		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).		Others
T16450	PDK1-IN-RS2		PDK
	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-selective PDK1 inhibitor (Kd: 9 μM).		PDK
T24741	RS1-PDK1 inhibitor	RS-1,RS1,RS 1	PDK
	RS1-PDK1 inhibitor (RS 1) is a selective inhibitor of the protein kinase PDK1 that can be used to treat and prevent disease or disorders.		PDK
T61339	LDHA/PDKs-IN-1
	LDHA/PDKs-IN-1 (compound 20e) is a highly effective dual inhibitor of PDKs and LDHA, displaying IC50 values of 0.8 μM and 0.15 μM, respectively. It significantly suppresses A549 cell proliferation (EC50 = 13.2 μM), reduc...
T60995	LDHA/PDKs-IN-2
	LDHA/PDKs-IN-2 (compound 20k) is a potent LDHA and PDKs dual inhibitor with IC50 values of 0.7 and 1.6 μM, respectively. LDHA/PDKs-IN-2 increases oxygen consumption as well as decreases the lactate formation. LDHA/PDKs-I...
T74814	PKM2/PDK1-IN-1
	PKM2/PDK1-IN-1, a shikonin thioether derivative, serves as a dual inhibitor for PKM2/PDK1. This compound effectively inhibits the proliferation and induces apoptosis in NSCLC cells. It promotes intercellular ROS producti...
T17224	VER-246608		Dehydrogenase , PDK
	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-4, respectively).VER-246608 disrupts Warburg metabolism an...		Dehydrogenase , PDK
T22350	JX06		Apoptosis , Dehydrogenase , PDK
	JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.		Apoptosis , Dehydrogenase , PDK
T11765	KPLH1130		Dehydrogenase , PDK
	KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.		Dehydrogenase , PDK
T19783	Dehydroabiethylamine	NSC-2955,NSC 2955,Dehydroabietylamine,NSC2955,Leelamine free base,Leelamine	P450 , PDK
	Dehydroabiethylamine (NSC-2955) is an inducer of hepatic CYP2B activity. Dehydroabiethylamine inhibits pyruvate dehydrogenase kinases (PDKs) and intracellular cholesterol transport with anti-tumor activity.		P450 , PDK
T12566	PS10		PDK
	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).		PDK

Compounds

Target: Apoptosis, VEGFR, PKA, Chk, CDK, PDK

BX795

T1830

Synonym:

Target: IκB/IKK, Chk, CDK, c-Kit, PDK, Autophagy

Synonym: PDK1 inhibitor 2,BX 517,BX-517

Synonym: PDK1 inhibitor

Target: PDK

PDK4-IN-1 hydrochloride

T12412L

Synonym:

Target: Apoptosis, PDK

Synonym: RS-1,RS1,RS 1

Target: Dehydrogenase, PDK

JX06

T22350

Synonym:

Target: Apoptosis, Dehydrogenase, PDK

KPLH1130

T11765

Synonym:

Target: Dehydrogenase, PDK

Dehydroabiethylamine

T19783

Synonym: NSC-2955,NSC 2955,Dehydroabietylamine,NSC2955,Leelamine free base,Leelamine

カタログ番号	製品名	別名	ターゲット
T3895	Polyphyllin I		Apoptosis , Akt , JNK , PDK , mTOR , Autophagy
	Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D ha...		Apoptosis , Akt , JNK , PDK , mTOR , Autophagy
T3604	Sodium dichloroacetate	Sodium Dichloroacetate,DCA,BCA,bichloroacetic acid,Sodium dichloroacetate (DCA)	Apoptosis , Dehydrogenase , Reactive Oxygen Species , PDK
	Sodium dichloroacetate (BCA) , 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 derepress a mitochondrial potassium-ion chann...		Apoptosis , Dehydrogenase , Reactive Oxygen Species , PDK

天然物製品

Polyphyllin I

T3895

Synonym:

Target: Apoptosis, Akt, JNK, PDK, mTOR, Autophagy

Sodium dichloroacetate

T3604

Synonym: Sodium Dichloroacetate,DCA,BCA,bichloroacetic acid,Sodium dichloroacetate (DCA)

Target: Apoptosis, Dehydrogenase, Reactive Oxygen Species, PDK

Recombinant Proteins

Species：

Expression System：

Tag：

カタログ番号	製品名	Species	Expression System
TMPY-04568	PDK1 Protein, Human, Recombinant (His)	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 predominantl...
TMPH-00515	PPDK Protein, Entamoeba histolytica, Recombinant (His & SUMO)	Entamoeba histolytica	E. coli
	Catalyzes the reversible phosphorylation of pyruvate and phosphate. In E.histolytica and C.symbiosus, PPDK functions in the direction of ATP synthesis.
TMPY-04445	PDK4 Protein, Mouse, Recombinant (His & GST)	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...
TMPH-02469	PDK1 Protein, Mouse, Recombinant (His)	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-00422	Ppdk Protein, Clostridium symbiosum, Recombinant (His & Myc)	Clostridium symbiosum	E. coli
	Catalyzes the reversible phosphorylation of pyruvate and phosphate. In E.histolytica and C.symbiosus, PPDK functions in the direction of ATP synthesis. Ppdk Protein, Clostridium symbiosum, Recombinant (His & Myc) is expr...
TMPH-02470	PDK3 Protein, Mouse, Recombinant (His)	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.