PLK
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
PLK产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1109 |
BI 2536BI 2536是一种有效的Plk1抑制剂，无细胞试验中IC50为0.83 nM，比作用于Plk2和Plk3选择性分别高4和11倍。Phase 2。 |
(C) HeLa cells were treated with inhibitors of Aurora B (hesperadin), Aurora A (Aurora A inhibitor I), CDK1 (roscovitine), or PLK1 (BI2536) for 2 hours before immunostaining for tubulin and phosphorylated RV[S/T]F (p-RV[S/T]F). Nuclei are indicated with DAPI. Control cells were not treated with any inhibitor. More than 50 cells were imaged for each condition in three independent experiments. Scale bar, 20 μm.
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| S2235 |
Volasertib (BI 6727)Volasertib (BI 6727)是一种高度有效的Plk1抑制剂，无细胞试验中IC50为0.87 nM，比作用于Plk2和Plk3选择性高6和65倍。Phase 3。 |
Annexin V-PI staining flow cytometry analysis showing increased cell death in response to volasertib treatment (50 nmol/L 72 hours) in cisplatin-resistant EOC cells (OV231-CP30 and SKOV3-CP30) as compared with their cisplatin-sensitive counterparts (OV231 and SKOV3), respectively.
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| S1362 |
Rigosertib (ON-01910)Rigosertib (ON-01910)是一种非ATP竞争性PLK1抑制剂，无细胞试验中IC50为9 nM，比作用于Plk2选择性高30倍，对Plk3没有抑制活性。Phase 3。 |
(A) Rigosertib induced increased apoptosis in CD34+ cells from MDS patients. Especially those from high-grade MDS (Left), in a dose-dependent manner (Right); (B) rigosertib also induced increased apoptosis in MDS and leukemia cell lines, including MDS-L, SKM1, U937, K562, Kasumi-1 and KG1a (Left), in a dose-dependent manner (Right); (C) rigosertib could not induce apoptosis in CD34+ cells from normal controls; (D) the LD50 values were lower in patients with high-grade MDS than in those with low-grade MDS (left). Patients with a normal and abnormal karyotype did not differ;
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| S2193 |
GSK461364GSK461364抑制纯化的Plk1，无细胞试验中Ki为2 nM。比作用于Plk2/3选择性高1000倍。Phase 1。 |
Cells with decreased GRK5 expression are more sensitive to PLK1 inhibition.A , shown is cell death in control or GRK5-shRNA stably transfected cells after 72 h of treatment with 0-120 nM BI 2536 as determined by trypan blue exclusion (n = 6).B , shown is cell death in control or GRK5-shRNA stably transfected cells after 72 h treatment with 0 –120 nM GSK461364, as determined by trypan blue exclusion ( n = 4). |
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| S1485 |
HMN-214HMN-214是HMN-176的前体药物，改变了Plk1的细胞空间定位。 |
Intracellular trafficking of plasmid DNA in the presence and absence of PLK1 inhibitors. PC3-PSMA cells were transfected with polyplexes of PEI:fluorescein (green)-labeled plasmid DNA at a weight ratio of 1:4. Cells treated with A) vehicle control (DMSO) and B) 25 nM BI 2536 are shown 48 h after co-treatment with polyplexes. Cells treated with C) vehicle control (DMSO) and D) HMN-214 are shown 24 h after co-treatment with polyplexes. Scale bar = 20 μm. Blue signal indicates DAPI-stained nuclei, and white arrows indicate sequestration of plasmid DNA in the perinuclear recycling compartment (PNRC). Red arrows indicate altered plasmid DNA localization following treatment with PLK1 inhibitors. Images are representative of three independent experiments (N = 3). (For interpretation of the references to color in this figure legend, the reader is referred to the web version of this article.) |
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| S2898 |
MLN0905MLN0905是一种有效的PLK1抑制剂，IC50为2 nM。 |
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| S7248 |
Ro3280Ro3280是一种有效的，高选择性Polo-like kinase 1(PLK1)抑制剂，IC50为3 nM。 |
RO3280 promotes the formation of multinucleated cells in bladder cancer cell lines. (A) Representative images of cells stained with DAPI (blue) and alpha‐tubulin (red) were examined under a fluorescence microscope (magnification 400×). Enlarged cells containing multiple evenly stained nuclei (multinucleated cells) are characteristic of mitotic catastrophe (white arrow). (B) Quantification of the percentage of multinucleated cells based on fluorescence microscopy analysis (the data are presented as the mean ± S.E.M., *P < 0.05).
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| S7255 |
NMS-P937 (NMS1286937)NMS-P937（NMS1286937）是一种口服有效的，选择性Polo-like Kinase 1 (PLK1)抑制剂有,其IC50为2 nM，比PLK2/PLK3高出5000倍的选择性。第1阶段。 |
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| S7552 |
CFI-400945CFI-400945是一种具有口服活性的、有效的、选择性的PLK4抑制剂，Ki值为0.26 nM。 |
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| S7720 |
SBE 13 HClSBE 13 HCl是一种有效的选择性PLK1抑制剂，IC50为200 pM，选择性比 Aurora A 激酶, Plk2 和 Plk3高4000多倍。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1109 |
BI 2536BI 2536是一种有效的Plk1抑制剂，无细胞试验中IC50为0.83 nM，比作用于Plk2和Plk3选择性分别高4和11倍。Phase 2。 |
(C) HeLa cells were treated with inhibitors of Aurora B (hesperadin), Aurora A (Aurora A inhibitor I), CDK1 (roscovitine), or PLK1 (BI2536) for 2 hours before immunostaining for tubulin and phosphorylated RV[S/T]F (p-RV[S/T]F). Nuclei are indicated with DAPI. Control cells were not treated with any inhibitor. More than 50 cells were imaged for each condition in three independent experiments. Scale bar, 20 μm.
|
|
| S2235 |
Volasertib (BI 6727)Volasertib (BI 6727)是一种高度有效的Plk1抑制剂，无细胞试验中IC50为0.87 nM，比作用于Plk2和Plk3选择性高6和65倍。Phase 3。 |
Annexin V-PI staining flow cytometry analysis showing increased cell death in response to volasertib treatment (50 nmol/L 72 hours) in cisplatin-resistant EOC cells (OV231-CP30 and SKOV3-CP30) as compared with their cisplatin-sensitive counterparts (OV231 and SKOV3), respectively.
|
|
| S1362 |
Rigosertib (ON-01910)Rigosertib (ON-01910)是一种非ATP竞争性PLK1抑制剂，无细胞试验中IC50为9 nM，比作用于Plk2选择性高30倍，对Plk3没有抑制活性。Phase 3。 |
(A) Rigosertib induced increased apoptosis in CD34+ cells from MDS patients. Especially those from high-grade MDS (Left), in a dose-dependent manner (Right); (B) rigosertib also induced increased apoptosis in MDS and leukemia cell lines, including MDS-L, SKM1, U937, K562, Kasumi-1 and KG1a (Left), in a dose-dependent manner (Right); (C) rigosertib could not induce apoptosis in CD34+ cells from normal controls; (D) the LD50 values were lower in patients with high-grade MDS than in those with low-grade MDS (left). Patients with a normal and abnormal karyotype did not differ;
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| S2193 |
GSK461364GSK461364抑制纯化的Plk1，无细胞试验中Ki为2 nM。比作用于Plk2/3选择性高1000倍。Phase 1。 |
Cells with decreased GRK5 expression are more sensitive to PLK1 inhibition.A , shown is cell death in control or GRK5-shRNA stably transfected cells after 72 h of treatment with 0-120 nM BI 2536 as determined by trypan blue exclusion (n = 6).B , shown is cell death in control or GRK5-shRNA stably transfected cells after 72 h treatment with 0 –120 nM GSK461364, as determined by trypan blue exclusion ( n = 4). |
|
| S1485 |
HMN-214HMN-214是HMN-176的前体药物，改变了Plk1的细胞空间定位。 |
Intracellular trafficking of plasmid DNA in the presence and absence of PLK1 inhibitors. PC3-PSMA cells were transfected with polyplexes of PEI:fluorescein (green)-labeled plasmid DNA at a weight ratio of 1:4. Cells treated with A) vehicle control (DMSO) and B) 25 nM BI 2536 are shown 48 h after co-treatment with polyplexes. Cells treated with C) vehicle control (DMSO) and D) HMN-214 are shown 24 h after co-treatment with polyplexes. Scale bar = 20 μm. Blue signal indicates DAPI-stained nuclei, and white arrows indicate sequestration of plasmid DNA in the perinuclear recycling compartment (PNRC). Red arrows indicate altered plasmid DNA localization following treatment with PLK1 inhibitors. Images are representative of three independent experiments (N = 3). (For interpretation of the references to color in this figure legend, the reader is referred to the web version of this article.) |
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| S2898 |
MLN0905MLN0905是一种有效的PLK1抑制剂，IC50为2 nM。 |
||
| S7248 |
Ro3280Ro3280是一种有效的，高选择性Polo-like kinase 1(PLK1)抑制剂，IC50为3 nM。 |
RO3280 promotes the formation of multinucleated cells in bladder cancer cell lines. (A) Representative images of cells stained with DAPI (blue) and alpha‐tubulin (red) were examined under a fluorescence microscope (magnification 400×). Enlarged cells containing multiple evenly stained nuclei (multinucleated cells) are characteristic of mitotic catastrophe (white arrow). (B) Quantification of the percentage of multinucleated cells based on fluorescence microscopy analysis (the data are presented as the mean ± S.E.M., *P < 0.05).
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| S7255 |
NMS-P937 (NMS1286937)NMS-P937（NMS1286937）是一种口服有效的，选择性Polo-like Kinase 1 (PLK1)抑制剂有,其IC50为2 nM，比PLK2/PLK3高出5000倍的选择性。第1阶段。 |
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| S7552 |
CFI-400945CFI-400945是一种具有口服活性的、有效的、选择性的PLK4抑制剂，Ki值为0.26 nM。 |
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| S7720 |
SBE 13 HClSBE 13 HCl是一种有效的选择性PLK1抑制剂，IC50为200 pM，选择性比 Aurora A 激酶, Plk2 和 Plk3高4000多倍。 |
