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Search Results for " plk1 inhibitor "

55

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2704	MLN0905 PLK1 Inhibitor	PLK	Cell Cycle/Checkpoint
	MLN0905 (PLK1 Inhibitor) 是一种 PLK1的有效抑制剂，IC50值为 2 nM。
T21678	3MB-PP1	PLK	Cell Cycle/Checkpoint
	3MB-PP1是嘌呤类似物，是一种 Polo 样激酶 1 (Plk1) 抑制剂。在表达类似物敏感的 Plk1 等位基因的细胞中，3MB-PP1 通过靶向 Plk1 阻断有丝分裂进程和细胞分裂。3MB-PP1 特异性抑制类似物敏感的 Ssn3 (Cdk8)。3MB-PP1 抑制 Leu93 突变 Zipper-interacting protein kinase(Leu93-ZIPK)，IC50为2 μM。3MB-PP1 可用于细胞分裂和白色念珠菌 (Candida albicans) 菌丝形成的研究。
T25969	Poloxin-2 Poloxin2,Poloxin 2	PLK	Cell Cycle/Checkpoint
	Poloxin-2 是一种具有有效性和选择性的 Plk1 PBD 抑制剂，具有抗肿瘤活性，可降低HeLa细胞中Plk1的蛋白水平。
T15454	GW843682X GW843682	VEGFR; PLK; CDK; PDGFR; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
	GW843682X (GW843682) 是 PLK1 和 PLK3 的特异性和 ATP 竞争性抑制剂，IC50 分别为 2.2 nM 和 9.1 nM。
T1839	Mps1-IN-2	Kinesin; PLK	Cell Cycle/Checkpoint; Cytoskeletal Signaling
	Mps1-IN-2 是一种 ATP 竞争性Mps1/Plk1选择性双重抑制剂，对 Mps1 的IC50和Kd 值分别为 145 和 12 nM，对 Plk1 的Kd 值为 61 nM。
T2438	HMN-214 IVX-214,HMN214	PLK	Cell Cycle/Checkpoint
	HMN-214 (IVX-214) 是一种可口服的 HMN-176 前体药物，是一种有效的 PLK1 抑制剂，平均 IC50 为 0.12 μM，具有抗肿瘤活性。
T28904	T521 T 521	PLK	Cell Cycle/Checkpoint
	T521 是 Plk1 PBD 的选择性抑制剂，对 Plk2 和 Plk3 无抑制作用。
T2634	Ro3280 RO 3280,Ro5203280	PLK	Cell Cycle/Checkpoint
	Ro3280 (Ro5203280) 是一种高度选择性的PLK1抑制剂，IC50和Kd 值分别为 3 nM 和 0.09 nM。
T6173	BI 2536 4-[[(7R)-8-环戊基-7-乙基-5,6,7,8-四氢-5-甲基-6-氧代-2-喋啶基]氨基]-3-甲氧基-N-(1-甲基-4-哌啶基)苯甲酰胺	Apoptosis; Epigenetic Reader Domain; PLK	Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic
	BI 2536 一种是PLK1和BRD4的双抑制剂，IC50分别为 0.83 和 25 nM。它抑制 IFNB 干扰素 β 基因转录。
T22700	Cyclapolin 9	PLK	Cell Cycle/Checkpoint
	Cyclapolin 9 是一种具有选择性、有效性和 ATP 竞争性的 polo-like kinase 1 (PLK1) 抑制剂，IC50 为 500 nM，对其他激酶尚未显示出活性。
T2271	SBE13 Hydrochloride SBE 13 hydrochloride,SBE 13 HCl	Apoptosis; PLK; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint
	SBE13 Hydrochloride (SBE 13 HCl) 是一种选择性的Plk1抑制剂，IC50值为 0.2 nM，对 Plk2 的IC50>66 μM，Plk3的IC50值为875 nM。
T17008	TC-S 7005	PLK	Cell Cycle/Checkpoint
	TC-S 7005是一种有效的Polo 样激酶的抑制剂，Plk1、Plk2和Plk3的IC50值分别为214 nM，4 nM 和24 nM。
T6283	Wortmannin SL-2052,渥曼青霉素,KY-12420	ATM/ATR; DNA-PK; Serine/threonin kinase; PLK; PI3K; Antibiotic; Autophagy	Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling
	Wortmannin (SL-2052) 是一种 PI3K 抑制剂 (IC50=3 nM)，具有共价性和不可逆性。Wortmannin 也是一种 PlK1 和 PlK3 的抑制剂 (IC50=5.8/48 nM)，可以阻断自噬。
T6247	Onvansertib NMS-P937,NMS-1286937	Apoptosis; PLK	Apoptosis; Cell Cycle/Checkpoint
	Onvansertib (NMS-1286937) 是一种可口服的高选择性PLK1抑制剂，IC50值为 2 nM。
T71399	Plogosertib CYC140	PLK	Cell Cycle/Checkpoint
	Plogosertib (CYC140) 是一种具有口服活性、选择性、高效性和 ATP 竞争性的 PLK1 抑制剂，IC50 值为 3 nM。Plogosertib 具有抗增殖和抗癌活性，可用于研究实体瘤和血液肿瘤。
T5818	Rigosertib sodium Rigosertib,Estybon,ON-01910	Apoptosis; PLK; PI3K	Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling
	Rigosertib sodium (ON-01910) 是一种选择性的非 ATP 竞争性PLK1抑制剂，IC50值为 9 nM。它是一种多激酶抑制剂和选择性抗癌剂，通过抑制PI3K/Akt 途径诱导细胞凋亡，促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。
T16750	Rigosertib ON-01910,瑞格色替	Apoptosis; FLT; PLK; PI3K; Bcr-Abl; CDK; PDGFR; Src	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	Rigosertib (ON-01910) 是一种多激酶抑制剂和选择性抗癌剂，通过抑制 PI3K/Akt 途径诱导细胞凋亡，促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。它是一种选择性的非 ATP 竞争性PLK1抑制剂，IC50值为 9 nM。
T2458	CID755673	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	CID755673是一种高效选择性 PKD1抑制剂，IC50为182 nM。
T6338	PHA-680632 PHA 680632,PHA680632	FGFR; PLK; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
	PHA-680632 是一种极光激酶抑制剂，对极光激酶 A、B 和C 的IC50值分别为 27、135和 120 nM。它对 FGFR1、FLT3、LCK、PLK1、STLK2 和 VEGFR2/3 的 IC50 高 10 到 200 倍。
T7200	TAK-960	PLK	Cell Cycle/Checkpoint
	TAK-960 是选择性的 polo 样激酶 1 口服有效抑制剂，IC50为 0.8 nM，对 PLK2 和 PLK3 也有抑制作用，IC50分别为 16.9 和 50.2 nM。它抑制多种肿瘤细胞系的增殖，可治疗多种肿瘤异种移植。
T6458	CYC-116 噻氯匹定	VEGFR; FLT; CDK; S6 Kinase; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	CYC116是一种有效的极光激酶 A 和 B 的抑制剂，Ki 值分别为8和9 nM。
T6077	ZM-447439	Apoptosis; MEK; Src; Aurora Kinase	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; Tyrosine Kinase/Adaptors
	ZM 447439是一种极光激酶 (aurora) 抑制剂，对aurora A 和B 的IC50值分别为110和130 nM。
T6070	(E/Z)-Rigosertib sodium N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium	PLK	Cell Cycle/Checkpoint
	ON-01910 是一种非 ATP 竞争性 PLK1 抑制剂（IC50 为 9 nM，在无细胞试验中）。它对 Plk2 的选择性高出 30 倍，对 Plk3 没有活性。 Rigosertib 抑制 PI3K/Akt 通路并激活氧化应激信号。 Rigosertib 可诱导多种癌细胞凋亡。它是一种合成的苄基苯乙烯基砜类似物，具有潜在的抗肿瘤活性。
T6940	PHA-767491 hydrochloride CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride	Apoptosis; GSK-3; CDK	Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
	PHA-767491 hydrochloride (CAY-10572 hydrochloride) 是一种Cdc7-Dbf4(DDK)/Cdk9的双重抑制剂，IC50值分别为 10 nM 和 34 nM。
T6019	Volasertib BI 6727,伏拉塞替	Apoptosis; PLK	Apoptosis; Cell Cycle/Checkpoint
	Volasertib (BI 6727) 是一种具有口服活性的高效ATP 竞争性Polo 样激酶 1 抑制剂。它抑制 PLK2 和 PLK3，IC50分别为 5 和 56 nM。它是二氢蝶呤酮衍生物，有抗肿瘤活性，可诱导有丝分裂停滞和细胞凋亡。
T10215	AAPK-25	Apoptosis; PLK; Aurora Kinase	Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic
	AAPK-25 是选择性的Aurora/PLK 激酶双重抑制剂，显示出抗肿瘤活性。它可造成有丝分裂延迟并阻滞前中期细胞，通过生物标志物组蛋白 H3Ser10磷酸化反应，导致细胞凋亡激增。
T71718	Plk1 PBD-IN-143
	Plk1 PBD-IN-143 is a novel Inhibitor of the Polo-Box Domain of Polo-like Kinase 1 (Plk1 PBD).
T16559	Poloxime	PLK	Cell Cycle/Checkpoint
	Poloxime is a hydrolysis product of poloxin and is a non-ATP-competitive Plk1 inhibitor. It also has moderate Plk1 inhibitory activity.
T71156	Poloxipan
	Poloxipan is a potent and pan-specific PLK1 inhibitor. In vitro, Poloxipan has IC50 3.2 uM (Plk1); 1.7 uM (Plk2); and 3 uM (Plk3). Poloxipan showed minor inhibition over FHA dommain of Chk2, S2 domian of STAT1, STAT5b, Lck, etc.
T23849	CAP-53194 CAP 53194,CAP53194
	CAP-53194 is a selective Plk1 inhibitor.
T40265	PLK1-IN-2 PLK1-IN-2
	PLK1-IN-2 is a PLK1 kinase inhibitor with an IC 50 value of 0.384 μM.
T63886	PLK1-IN-4
	PLK1-IN-4 是有效的、选择性的 PLK1 抑制剂 (IC50<0.508 nM)。PLK1-IN-4 对多种癌细胞表现出广泛的抗增殖作用。PLK1-IN-4 能够将细胞周期阻滞在 G2/M 期，并诱导癌细胞凋亡 (apoptosis)。PLK1-IN-4 能够用于研究肝细胞癌。
T69496	MCC1019
	MCC1019 is a novel selective inhibitor of the Polo-box domain of Polo-like kinase 1 (PLK1).
T81440	PLK1-IN-7
	PLK1-IN-7（化合物30e）是一种效能高的PLK1抑制剂，具备优异的抗增殖和抗肿瘤特性，其IC50为0.66 nM。
T81441	PLK1/p38γ-IN-1	p38 MAPK	MAPK
	PLK1/p38γ-IN-1（化合物14）为PLK1与p38γ多靶点抑制剂，体外有效抑制人肝细胞癌与肝母细胞瘤细胞增殖。
T28498	rac-CCT-250863
	Rac-CCT-250863, a potent Nek2 inhibitor, exhibits selectivity for Nek2 over PLK1, MPS1, Cdk2 and Aurora A.
T74777	PLK1-IN-6
	PLK1-IN-6, 作为一种高效且选择性的PLK1抑制剂，其IC50值仅为0.45 nM，对癌细胞表现出显著的抗增殖活性。
T71556	MK-1496
	MK1496 is a n orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a n...
T68428	ZK-Thiazolidinone
	ZK-Thiazolidinone, also known as TAL, is an ATP-competitive inhibitor of PLK1. In vitro, ZK-Thiazolidinone counteracts the role of Plk1 in previously established functions, notably, sister chromatid separation, centrosome maturation, and bipolar spindle assembly. In vivo, ZK-Thiazolidinone selectively inhibits PLK1 and causes a prometaphase-like mitotic (G2–M) arrest. ZK-Thiazolidinone inhibits human PLK1 (IC50, 19± 12 nM) and various human and mouse tumor cell lines (IC50, 0.2–1.3 μM). ZK-Thiaz...
T73172	FOXM1-IN-1
	FOXM1-IN-1 是一种有效的 FOXM1抑制剂，IC50值为 2.65 µM。FOXM1-IN-1 显示出抗增殖活性。FOXM1-IN-1 降低FOXM1、PLK1、CDC25B 蛋白的表达。
T64058	PLK1/BRD4-IN-1
	PLK1/BRD4-IN-1 (9b) 是一个口服具有活力的 PLK1 (IC50: 22 nM) 和 BRD4 (IC50: 109 nM) 双重抑制剂。PLK1/BRD4-IN-1 能够诱导细胞凋亡，并使细胞周期阻滞 (cell cycle arrest)，将几种增殖相关癌基因的转录下调，并具有良好的体内抗肿瘤作用。
T70244	JRN73958
	JRN73958 is an important precursor for the synthesis of scytonemin, also called Reduced scytonemin. Scytonemin is a biological pigment synthesized by many strains of cyanobacteria, including Calothrix sp., Lyngbya aestuarii, and others. Scytonemin is also a potent PKL1 inhibitor, which inhibits cell proliferation and arrests cell cycle through downregulating Plk1 activity in many cancel cells. Scytonemin was able to inhibit the proliferation of three myeloma cells in a dose-dependent manner, whi...
T41100	Volasertib trihydrochloride BI6727trihydrochloride,伏拉塞替三盐酸盐
	Volasertib (BI 6727) trihydrochloride is a dihydropteridinone derivative that exhibits potent and selective inhibition of Polo-like kinase 1 (PLK1), PLK2, and PLK3. It acts as an orally active ATP-competitive inhibitor with an IC50 of 0.87 nM against PLK1. Additionally, Volasertib trihydrochloride demonstrates IC50 values of 5 nM and 56 nM against PLK2 and PLK3, respectively. Its mechanism of action includes inducing mitotic arrest and apoptosis. Furthermore, Volasertib trihydrochloride has been...
T68463	BI-4834
	BI-4834 is a potent and selective Polo-like kinase 1 (PLK1) inhibitor. BI-4834 is also analogue (or Me-Too) of BI-2536. In vitro test shows that BI 4834 inhibits PLK1 with IC50=7.6 nm, but with higher selectivity over the related enzyme PLK3 (IC50 198.4 nm) as BI-2536.
T62591	SBE13
	SBE13 是一种选择性的、有效的 Plk1 抑制剂 (IC50: 200 pM)。SBE13 对 Plk2 或 Plk3 的作用较弱，其 IC50 值分别为＞66 μM 和 875 nM。
T70977	JMN13497
	JMN13497 is an precursor compound to for synthesis of scytonemin. Scytonemin is a biological pigment synthesized by many strains of cyanobacteria, including Calothrix sp., Lyngbya aestuarii, and others. Scytonemin is also a potent PKL1 inhibitor, which inhibits cell proliferation and arrests cell cycle through downregulating Plk1 activity in many cancel cells. Scytonemin was able to inhibit the proliferation of three myeloma cells in a dose-dependent manner, while U266 was the most sensitive on...
T69296	PHA-680626
	PHA-680626 is a potent and selective PLK inhibitor. PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases. PHA-680626 inhibits Plk1 (IC50 = 0.53 μM), Plk2 (IC50 = 0.07 μM) and Plk3 (IC50 = 1.61 μM).
T11573	HPN-01	Others	Others
	HPN-01 is a selective IKK inhibitor (pIC50s: 6.4, 7.0, and <4.8 for IKK-α, IKK-β, and IKK-ε). HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, ErbB2, EGFR, GSK3β, Src, PLK1, and VEGFR-2.
T61061	JH295 hydrate
	JH295 hydrate 通过 Cys22 烷基化从而抑制细胞Nek2，它是有效的，不可逆和选择性的NIMA 相关激酶 2 (Nek2)抑制剂 (IC50 = 770 nM)。JH295 hydrate 对有丝分裂激酶 Cdk1，Aurora B 或 Plk1 不具有活性，不干扰双极纺锤体组件或纺锤体组件检查点。
T64216	TAK-960 hydrochloride
	TAK-960 hydrochloride 是一种有效的、选择性的、口服具有活力的 polo-like kinase 1 (PLK1) 抑制剂 (IC50: 0.8 nM)。TAK-960 hydrochloride 也能够抑制 PLK2 (IC50: 16.9 nM) 和 PLK3 (IC50: 50.2 nM)。TAK-960 hydrochloride 能够抑制多种肿瘤细胞系的增殖，显著治疗多种肿瘤异种移植。

化合物

Cat.No: T2704

Synonym: PLK1 Inhibitor

Target: PLK

Cat.No: T21678

Target: PLK

Cat.No: T25969

Synonym: Poloxin2,Poloxin 2

Target: PLK

Cat.No: T15454

Synonym: GW843682

Target: VEGFR, PLK, CDK, PDGFR, Aurora Kinase

Cat.No: T1839

Target: Kinesin, PLK

Cat.No: T2438

Synonym: IVX-214,HMN214

Target: PLK

Cat.No: T28904

Synonym: T 521

Target: PLK

Cat.No: T2634

Synonym: RO 3280,Ro5203280

Target: PLK

Cat.No: T6173

Synonym: 4-[[(7R)-8-环戊基-7-乙基-5,6,7,8-四氢-5-甲基-6-氧代-2-喋啶基]氨基]-3-甲氧基-N-(1-甲基-4-哌啶基)苯甲酰胺

Target: Apoptosis, Epigenetic Reader Domain, PLK

Cat.No: T22700

Target: PLK

SBE13 Hydrochloride

Cat.No: T2271

Synonym: SBE 13 hydrochloride,SBE 13 HCl

Target: Apoptosis, PLK, Autophagy

Cat.No: T17008

Target: PLK

Cat.No: T6283

Synonym: SL-2052,渥曼青霉素,KY-12420

Target: ATM/ATR, DNA-PK, Serine/threonin kinase, PLK, PI3K, Antibiotic, Autophagy

Cat.No: T6247

Synonym: NMS-P937,NMS-1286937

Target: Apoptosis, PLK

Cat.No: T71399

Synonym: CYC140

Target: PLK

Rigosertib sodium

Cat.No: T5818

Synonym: Rigosertib,Estybon,ON-01910

Target: Apoptosis, PLK, PI3K

Cat.No: T16750

Synonym: ON-01910,瑞格色替

Target: Apoptosis, FLT, PLK, PI3K, Bcr-Abl, CDK, PDGFR, Src

Cat.No: T2458

Target: Serine/threonin kinase

Cat.No: T6338

Synonym: PHA 680632,PHA680632

Target: FGFR, PLK, Aurora Kinase

Cat.No: T7200

Target: PLK

Cat.No: T6458

Synonym: 噻氯匹定

Target: VEGFR, FLT, CDK, S6 Kinase, Aurora Kinase

Cat.No: T6077

Target: Apoptosis, MEK, Src, Aurora Kinase

(E/Z)-Rigosertib sodium

Cat.No: T6070

Synonym: N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium

Target: PLK

PHA-767491 hydrochloride

Cat.No: T6940

Synonym: CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride

Target: Apoptosis, GSK-3, CDK

Cat.No: T6019

Synonym: BI 6727,伏拉塞替

Target: Apoptosis, PLK

Cat.No: T10215

Target: Apoptosis, PLK, Aurora Kinase

Plk1 PBD-IN-143

Cat.No: T71718

Cat.No: T16559

Target: PLK

Cat.No: T71156

Cat.No: T23849

Synonym: CAP 53194,CAP53194

Cat.No: T40265

Synonym: PLK1-IN-2

Cat.No: T63886

Cat.No: T69496

Cat.No: T81440

PLK1/p38γ-IN-1

Cat.No: T81441

Target: p38 MAPK

Cat.No: T28498

Cat.No: T74777

Cat.No: T71556

ZK-Thiazolidinone

Cat.No: T68428

Cat.No: T73172

PLK1/BRD4-IN-1

Cat.No: T64058

Cat.No: T70244

Volasertib trihydrochloride

Cat.No: T41100

Synonym: BI6727trihydrochloride,伏拉塞替三盐酸盐

Cat.No: T68463

Cat.No: T62591

Cat.No: T70977

Cat.No: T69296

Cat.No: T11573

Target: Others

Cat.No: T61061

TAK-960 hydrochloride

Cat.No: T64216

Cat. No.	Product Name	Target	Signaling Pathways
TN3848	Dihydrobaicalein	PLK	Cell Cycle/Checkpoint
	Dihydrobaicalein 是一种来自黄芩的天然产物，一种PLK1抑制剂（IC50:6.3μM）。Dihydrobaicalein 对VRK2和PLK2有抑制作用。
T70495	Scytonemin
	Scytonemin is a biological pigment synthesized by many strains of cyanobacteria, including Calothrix sp., Lyngbya aestuarii, and others. Scytonemin is also a potent PKL1 inhibitor, which inhibits cell proliferation and arrests cell cycle through downregulating Plk1 activity in many cancel cells. Scytonemin was able to inhibit the proliferation of three myeloma cells in a dose-dependent manner, while U266 was the most sensitive one to scytonemin. Scytonemin , representing a novel Plk1 inhibitor, ...

天然产物

Dihydrobaicalein

Cat.No: TN3848

Target: PLK

Cat.No: T70495

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