65
3
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。 | |||
T40265 |
PLK1-IN-2
PLK1-IN-2 |
||
PLK1-IN-2 is a PLK1 kinase inhibitor with an IC 50 value of 0.384 μM. | |||
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). | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T6282 |
GSK461364
GSK461364A |
PLK | Cell Cycle/Checkpoint |
GSK461364 (GSK461364A) 是一种选择性,ATP 竞争性的PLK1可逆抑制剂,Ki 值为 2.2 nM。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T8912 |
5-ETHYL-4,5,6,7-TETRAHYDRO-THIAZOLO[5,4-C]PYRIDIN-2-YLAMINE
5-乙基-4,5,6,7-四氢-噻唑并[5,4-C]吡啶-2-胺 |
PLK | Cell Cycle/Checkpoint |
5-ETHYL-4,5,6,7-TETRAHYDRO-THIAZOLO[5,4-C]PYRIDIN-2-YLAMINE 靶向 PLK1。 | |||
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。 | |||
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。 | |||
T3643 |
HMN-176
|
PLK | Cell Cycle/Checkpoint |
HMN176 是一种二苯乙烯衍生物,可抑制有丝分裂,干扰 polo 样激酶-1 (PLK1) | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T41163 |
ZNL 02-096
Pomalidomide-C3-adavosertib |
Apoptosis; Wee1 | Apoptosis; Cell Cycle/Checkpoint |
ZNL 02-096 (Pomalidomide-C3-adavosertib) 是一种快速和选择性的 Wee1 降解剂 (IC50=3.58 nM)。ZNL 02-096 可在亚摩尔浓度下选择性降解 Wee1,而不损伤 AZD 1775 的二级靶点 PLK1。在体外 MOLT-4 细胞中,ZNL 02-096 可诱导 Wee1 降解、DNA 损伤积累、细胞周期停滞在 G2/M 期和细胞凋亡。ZNL 02-096 在 300 种癌症细胞系中显示出抗增殖作用。 | |||
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。 | |||
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. | |||
T68428 |
ZK-Thiazolidinone
|
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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... | |||
T69496 |
MCC1019
|
||
MCC1019 is a novel selective inhibitor of the Polo-box domain of Polo-like kinase 1 (PLK1). | |||
T28498 |
rac-CCT-250863
|
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Rac-CCT-250863, a potent Nek2 inhibitor, exhibits selectivity for Nek2 over PLK1, MPS1, Cdk2 and Aurora A. | |||
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... | |||
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... | |||
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... | |||
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。 | |||
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. | |||
T78986 |
MDEG-541
|
c-Myc | Cell Cycle/Checkpoint |
MDEG-541为一有效MYC-MAX降解剂,展现出显著的抗增殖活性,并有效降低GSPT1、MYC、GSPT2、PLK1蛋白表达水平。 | |||
T68686 |
DAP-81
|
||
DAP-81 is a diaminopyrimidine derivative that targets PLKs, destabilizing kinetochore microtubules. Other spindle tubules are stabilized, resulting in monopolar mitotic spindles. In vitro, DAP-81 inhibits Plk1 at an IC50 of 0.9 nM. DAP-81 is currently in ongoing preclinical evaluations. |
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。 | |||
TL0017 |
Aristolactam AIIIa
|
MAPK; CDK | Cell Cycle/Checkpoint; MAPK |
Aristolactam AIIIa is a new type of Plk1 inhibitors, targeting the Polo Box domain (PBD), it has anti-tumor activity. Aristolactam IIIa shows inhibition of platelet aggregation induced by collagen or arachidonic acid. | |||
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, ... |