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
| 目录号 | 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。BI-2536可抑制 Bromodomain 4 (BRD4) ，其Kd值为37 nM，并有效地抑制 c-Myc 的表达。BI-2536可诱导凋亡而减弱自噬。Phase 2。 |
|
|
| 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。Volasertib可在多种癌细胞中诱导细胞周期停滞和自噬。Phase 3。 |
Western blot analysis. HeLa or MCF7 cells were treated with nocodazole (noc, 50 ng/ml), paclitaxel (pacli, 50 nM), the Plk1 inhibitor BI 2536 (50 nM) or BI 6727 (50 nM) for 16 h and cellular extracts were prepared for western blot analysis with antibodies as indicated. con: cellular extracts from control cells without any treatment. β-actin served as loading control. |
|
| S2758 |
WortmanninWortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。Wortmannin 可抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。 |
L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment. |
|
| 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。Rigosertib 可抑制 PI3K/Akt 信号通路并激活氧化应激信号。Rigosertib 可诱导多种癌细胞的凋亡。Phase 3。 |
Along with cell death, immunoblotting shows ON 01910.Na induces hyperphosphorylation of RanGAP1, increased expression of RanGAP1.SUMO1 but decreased expression of free unmodified RanGAP1. No viable SU-DHL-5 cells were available for immunoblotting at 0.5 uM of ON 01910.Na.
|
|
| 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.) |
|
| 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).
|
|
| S5807 |
HMN-176HMN-176是HMN-214的活性代谢物，HMN-214在小鼠异种移植瘤模型中具有有效的抗肿瘤活性。 |
||
| S7255 |
onvansertib (NMS-P937)onvansertib (NMS-P937) 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。Phase 1。 |
||
| 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。 |
||
| 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。 |
| 目录号 | 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。BI-2536可抑制 Bromodomain 4 (BRD4) ，其Kd值为37 nM，并有效地抑制 c-Myc 的表达。BI-2536可诱导凋亡而减弱自噬。Phase 2。 |
|
|
| 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。Volasertib可在多种癌细胞中诱导细胞周期停滞和自噬。Phase 3。 |
Western blot analysis. HeLa or MCF7 cells were treated with nocodazole (noc, 50 ng/ml), paclitaxel (pacli, 50 nM), the Plk1 inhibitor BI 2536 (50 nM) or BI 6727 (50 nM) for 16 h and cellular extracts were prepared for western blot analysis with antibodies as indicated. con: cellular extracts from control cells without any treatment. β-actin served as loading control. |
|
| S2758 |
WortmanninWortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。Wortmannin 可抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。 |
L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment. |
|
| 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。Rigosertib 可抑制 PI3K/Akt 信号通路并激活氧化应激信号。Rigosertib 可诱导多种癌细胞的凋亡。Phase 3。 |
Along with cell death, immunoblotting shows ON 01910.Na induces hyperphosphorylation of RanGAP1, increased expression of RanGAP1.SUMO1 but decreased expression of free unmodified RanGAP1. No viable SU-DHL-5 cells were available for immunoblotting at 0.5 uM of ON 01910.Na.
|
|
| 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.) |
|
| 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).
|
|
| S5807 |
HMN-176HMN-176是HMN-214的活性代谢物，HMN-214在小鼠异种移植瘤模型中具有有效的抗肿瘤活性。 |
||
| S7255 |
onvansertib (NMS-P937)onvansertib (NMS-P937) 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。Phase 1。 |
||
| 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。 |
||
| 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。 |
沪公网安备 31011502012800号