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Search Results for " pdk1 "

Targets Recommended: PDK

35

抑制剂 & 化合物

2

天然产物

3

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T12398	MP7 PDK1 抑制剂,PDK1 inhibitor	PDK	PI3K/Akt/mTOR signaling
	MP7 (PDK1 inhibitor) 是磷酸肌醇依赖性激酶-1 (PDK1) 抑制剂。
T24741	RS1-PDK1 inhibitor RS-1,RS1,RS 1	PDK	PI3K/Akt/mTOR signaling
	RS1-PDK1 inhibitor (RS 1) 是一种选择性的蛋白激酶PDK1抑制剂，可用来治疗和预防疾病或失调。
T4046	BX517 PDK1 inhibitor 2,BX 517,BX-517	Akt; PDK	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	BX517 (PDK1 inhibitor 2) 是一种选择性 PDK1抑制剂，其 IC50=6 nM。
T16450	PDK1-IN-RS2	PDK	PI3K/Akt/mTOR signaling
	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).
T74814	PKM2/PDK1-IN-1	Others	Others
	PKM2/PDK1-IN-1 是一种紫草素硫醚衍生物，是PKM2/PDK1的双重抑制剂。 PKM2/PDK1-IN-1抑制NSCLC 细胞的增殖，并诱导细胞凋亡 (apoptosis)。 PKM2/PDK1-IN-1 诱导细胞间 ROS 产生，调节凋亡蛋白，参与线粒体和死亡受体通路。
T16670	PS210	PDK	PI3K/Akt/mTOR signaling
	PS210 是针对 PDK1的 PIF 结合口袋的、选择性的、有效的 PDK1激活剂，对其他蛋白激酶无活性。在细胞中，它的前药 PS423 可作为 PDK1的底物选择性抑制剂，抑制 S6K 的磷酸化和活化。
T1830	BX795	IκB/IKK; Chk; CDK; c-Kit; PDK; Autophagy	Autophagy; Cell Cycle/Checkpoint; NF-κB; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	BX795 是一种选择性PDK1抑制剂，也是相对特异性的TBK1和IKKɛ 抑制剂。它抑制 S6K1，Akt，PKCδ 和 GSK3β 的磷酸化，可调节自噬。
T1837	BX-912	Apoptosis; VEGFR; PKA; Chk; CDK; PDK	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	BX-912 是一种直接的，选择性的，ATP 竞争性的PDK1抑制剂，IC50值为 26 nM。它阻断肿瘤细胞 PDK1/Akt 信号转导，抑制多种肿瘤细胞株的锚定依赖性生长或诱导凋亡。
T2466	Osu03012 Osu-03012,Osu 03012,AR-12	PDK	PI3K/Akt/mTOR signaling
	Osu03012 (AR-12) 是一种口服生物可利用的小分子塞来昔布衍生的磷酸肌醇依赖性激酶 1(PDK1) 抑制剂，具有潜在的抗肿瘤活性。
T2348	GSK2334470	PDK	PI3K/Akt/mTOR signaling
	GSK2334470是一种高效的、特异性的PDK1抑制剂，IC50=10 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。
T3163	PS 48	PDK	PI3K/Akt/mTOR signaling
	PS 48 已被证明是一种 PKB 激酶 (PDK1) 激活剂 (Kd: 10.3 μM)。该化合物选择性地与 PKB 激酶 (PDK1) 的 PIF 结合口袋结合。
T24677	PS47 PS 47,PS-47	PDK	PI3K/Akt/mTOR signaling
	PS-47(PS 47) 是一种 PS48 的非活性 E-异构体。其中 PS48 是一种 PDK1 的激活剂。PS47 (PS 47) 可用作 PS48 的阴性对照。
T28218	NU6102 NU-6102,NU 6102	CDK	Cell Cycle/Checkpoint
	NU6102 是一种具有选择性和有效性的 ATP 竞争性 CDK2 抑制剂，具有抗肿瘤活性，对 CDK1/cyclinB、CDK2/cyclinA3、CDK1/CDK2、 CDK4、DYRK1A 、PDK1、ROCKII 具有抑制作用，可用于研究直肠癌。
T77685	6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile	PDK	PI3K/Akt/mTOR signaling
	6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile 是一种 PDK1 抑制剂，具有抗癌和抗增殖活性，可用来研究血管肉瘤、腺癌、多骨髓瘤、牛皮癣、前列腺癌和和阿尔茨海默病。
T12639	(R)-PS210	Others	Others
	(R)-PS210, the R enantiomer of PS210 is a substrate-selective allosteric PDK1 activator with an (AC50 of 1.8 μM).
T12566	PS10	PDK	PI3K/Akt/mTOR signaling
	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).
T70911	PF-5177624	Others	Others
	PF-5177624 is a selective and potent PDK1 inhibitor inducing anti-tumor activity in breast cancer cells.
T23495	UCN-01	Others	Others
	inhibitor of Akt, protein kinase C, PDK1 and cyclin-dependent kinases
T2420	PHT-427 PHT 427,CS-0223	Apoptosis; Akt; PDK	Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	PHT-427 (CS-0223) 是一种 Akt 和 PDPK1双重抑制剂，与 Akt 和 PDPK1 中的 PH 结构域有亲和性，Ki 分别为 2.7 μM 和 5.2 μM。
T24676	PS423 PS210AM,PS 210 AM,PS 423,PS210-AM,PS-423	Others	Others
	PS423 is a substrate-selective protein kinase PDK1 inhibitor that acts by binding to the PIF-pocket allosteric docking site.
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。
T24753	SA-16 SA 16	Others	Others
	SA-16 is a potent dual inhibitor of PDK1 and Aurora kinase.
T10890	CRTh2 antagonist 3	Others	Others
	CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has the
T60524	HIF-1α-IN-4	Others	Others
	HIF-1α-IN-4 是 HIF-1α抑制剂，在 HEK293T 细胞中的IC50值为 24 nM，具有潜在的抗肿瘤作用。 HIF-1α-IN-4 在缺氧条件下下调 VEGF 和 PDK1 mRNA 的表达。
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。
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。
T37561	BX-320	Others	Others
	BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50= 30 nM).1It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 μM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 μM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 μM). BX-3...
T60532	HIF-1α-IN-5	Others	Others
	HIF-1α-IN-5 是 HIF-1α的抑制剂，在 HEK293T 细胞中的 IC50值为 24 nM，也可抑制 MAO-A 的活性。在缺氧条件下， HIF-1α-IN-5可下调 VEGF 和 PDK1 mRNA 的表达。HIF-1α-IN-5 具有用于癌症研究的潜力。
T38263	TBK1/IKKε-IN-4 TBK1/IKKε-IN-4	Others	Others
	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]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IK...
T79723	PDK-IN-2	Others	Others
	PDK-IN-2（Compound 1F）是一种具有IC50为68 nM的PDK抑制剂。该化合物能够抑制PDK1和PDK4在细胞内的表达，增强线粒体生物能并降低糖酵解表型，同时诱导细胞走向线粒体途径的apoptosis。此外，PDK-IN-2在4T1同基因小鼠模型中能够有效抑制肿瘤生长。
T81446	PKM2 activator 6	Others	Others
	PKM2 activator 6 (Compound Z10) 作为一种PKM2激活剂同时抑制PDK1，其KD值分别为121 μM和19.6 μM。该化合物诱导结直肠细胞发生凋亡，并显著抑制细胞增殖与迁移。通过抑制糖酵解作用，PKM2 activator 6降低DLD-1、HCT-8、HT-29、MCF-10A细胞的增殖，IC50值分别为10.04、2.16、3.57、66.39 μM。
T35491	3,5-dimethyl PIT-1	Others	Others
	PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorab...
T84871	Emetine hydrochloride NSC 33669	Others	Others
	Emetine hydrochloride (NSC 33669)，一种从ipecac根部提取的生物碱，用于临床上作为催吐及抗原生动物药物。它能够降低HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2)和BRD4，抑制细胞自噬，并展现抗疟疾、抗病毒、抗细菌及抗变形虫效果。
TQ0313	NVP-BAG956 BAG956	PI3K	PI3K/Akt/mTOR signaling
	NVP-BAG956 is an ATP-competitive PI3K inhibitor (IC50s: 34/56/112/444 nM for PI3Kδ/PI3Kα/PI3Kγ/PI3Kβ).

化合物

Cat.No: T12398

Synonym: PDK1 抑制剂,PDK1 inhibitor

Target: PDK

RS1-PDK1 inhibitor

Cat.No: T24741

Synonym: RS-1,RS1,RS 1

Target: PDK

Cat.No: T4046

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

Target: Akt, PDK

Cat.No: T16450

Target: PDK

PKM2/PDK1-IN-1

Cat.No: T74814

Target: Others

Cat.No: T16670

Target: PDK

Cat.No: T1830

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

Cat.No: T1837

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

Cat.No: T2466

Synonym: Osu-03012,Osu 03012,AR-12

Target: PDK

Cat.No: T2348

Target: PDK

Cat.No: T22350

Target: Apoptosis, Dehydrogenase, PDK

Cat.No: T3163

Target: PDK

Cat.No: T24677

Synonym: PS 47,PS-47

Target: PDK

Cat.No: T28218

Synonym: NU-6102,NU 6102

Target: CDK

6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile

Cat.No: T77685

Target: PDK

Cat.No: T12639

Target: Others

Cat.No: T12566

Target: PDK

Cat.No: T70911

Target: Others

Cat.No: T23495

Target: Others

Cat.No: T2420

Synonym: PHT 427,CS-0223

Target: Apoptosis, Akt, PDK

Cat.No: T24676

Synonym: PS210AM,PS 210 AM,PS 423,PS210-AM,PS-423

Target: Others

Cat.No: T81788

Target: Others

Cat.No: T24753

Synonym: SA 16

Target: Others

CRTh2 antagonist 3

Cat.No: T10890

Target: Others

Cat.No: T60524

Target: Others

Cat.No: T17224

Target: Dehydrogenase, PDK

Cat.No: T74830

Target: Others

Cat.No: T37561

Target: Others

Cat.No: T60532

Target: Others

TBK1/IKKε-IN-4

Cat.No: T38263

Synonym: TBK1/IKKε-IN-4

Target: Others

Cat.No: T79723

Target: Others

PKM2 activator 6

Cat.No: T81446

Target: Others

3,5-dimethyl PIT-1

Cat.No: T35491

Target: Others

Emetine hydrochloride

Cat.No: T84871

Synonym: NSC 33669

Target: Others

Cat.No: TQ0313

Synonym: BAG956

Target: PI3K

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。
T3895	Polyphyllin I 重楼皂苷I,重楼皂甙	Apoptosis; Akt; JNK; PDK; mTOR; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling
	Polyphyllin I 是从七叶一枝花中提取的生物活性成分，具有很强的抗肿瘤活性。它是 JNK 信号通路的激活剂，也是 PDK1/Akt/mTOR 信号传导的抑制剂。它诱导自噬，G2/M 期阻滞和细胞凋亡。

天然产物

Cat.No: T0809

Synonym: Dicumarol,双羟香豆素,双香豆素

Target: Dehydrogenase, NADPH, PDK

Cat.No: T3895

Synonym: 重楼皂苷I,重楼皂甙

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

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPH-02469	PDK1 Protein, Mouse, Recombinant (His) Pdk1,Pyruvate dehydrogenase kinase isoform...	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.
TMPY-04568	PDK1 Protein, Human, Recombinant (His) pyruvate dehydrogenase kinase, isozyme 1,PDHK1<...	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-04392	RSK3 Protein, Human, Recombinant (GST) HU-2,ribosomal protein S6 kinase, 90kDa, polypeptide 2,S6K-α...	Human	Baculovirus Insect Cells
	Ribosomal protein S6 kinase alpha-2, also known as 9 kDa ribosomal protein S6 kinase 2, MAP kinase-activated protein kinase 1c, MAPK-activated protein kinase 1c, Ribosomal S6 kinase 3, RSK-3, RPS6KA2 and MAPKAPK1C, is a nucleus protein that belongs to the protein kinase superfamily, AGC Ser/Thr protein kinase family and S6 kinase subfamily. RPS6KA2 / RSK-3 is expressed in many tissues. Highest expression is in lung and skeletal muscle. The expression of RPS6KA2 reduced proliferation, caused G1 a...

重组蛋白

PDK1 Protein, Mouse, Recombinant (His)

Cat.No: TMPH-02469

Species: Mouse

Expression System: Baculovirus Insect Cells

PDK1 Protein, Human, Recombinant (His)

Cat.No: TMPY-04568

Species: Human

Expression System: Baculovirus Insect Cells

RSK3 Protein, Human, Recombinant (GST)

Cat.No: TMPY-04392

Species: Human

Expression System: Baculovirus Insect Cells

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