Kinesin
信号通路图
研究领域
抑制剂选择性比较
Kinesin产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1452 |
Ispinesib (SB-715992)Ispinesib (SB-715992)是一种有效的，特异性的，可逆kinesin spindle protein (KSP)抑制剂，无细胞试验中Kiapp为1.7 nM，对CENP-E， RabK6， MCAK， MKLP1，KHC和Kif1A没有抑制作用。Ispinesib可诱导有丝分裂阻滞和细胞的凋亡。Phase 2。 |
Representative photographs of fluorescent staining of microtubules and nuclei in MDA-MB-231 cells 24 h post-treatment with 4 nM of ispinesib or vinblastine or their combination. Arrows and arrowheads denote mitotic cells with monoploar and bipolar spindles, respectively. Scale bars, 20 um.
|
|
| S2182 |
SB743921 HClSB743921是一种kinesin spindle protein (KSP)（纺锤体驱动蛋白）抑制剂，Ki为0.1 nM，对MKLP1， Kin2， Kif1A， Kif15， KHC， Kif4和CENP-E几乎没有亲和力。Phase 1/2。 |
HeLa cells expressing iRFP were seeded onto 96-well plates and incubated with buffer or different concentrations of SB743921.During the next five days, the plate was scanned with an infrared imaging system (upper panel) to quantify the infrared signals (lower panel). |
|
| S2731 |
AZ 3146AZ 3146是一种选择性Mps1抑制剂，IC50为35 nM左右，有助于聚集CENP-E(驱动蛋白相关的动力蛋白)，对FAK， JNK1， JNK2和Kit作用效果稍弱。 |
Dose response curves for the treatment of breast cancer cell lines in the absence or presence of escalating doses of the TTK inhibitor (TTKi) AZ3146. The survival of cells was measured using the CellTitre MTS/MTA assay carried out 6 days after treatment. Percentage survival (n ¼ 3 per dose) was calculated as the percentage of the signal from treated cells to that from control cells. |
|
| S7090 |
GSK923295GSK923295是一级特异性变构抑制剂CENP-E驱动蛋白ATPase的变构抑制剂，Ki为3.2 nM，对突变型I182和T183作用效果稍弱。Phase 1。 |
(f) HeLa cells were treated with mitotic kinesin CENP-E inhibitor GSK923295 (50 nM) for 1 h to generate misaligned kinetochores. After fixation, cells were stained for ACA, tubulin, and TIP60. Statistical significance was tested by two-sided t-test and represented by asterisks corresponding to ***, p < 0.001. Scale bars, 5 μm. |
|
| S7355 |
ARQ 621ARQ621是一种变构选择性的Eg5 mitotic motor protein抑制剂。第1阶段。 |
||
| S8257New |
CFI-402257CFI-402257 is a potent highly selective, and orally active small-molecule inhibitor of Mps1 with Ki value of 0.09 ± 0.02 nM. |
||
| S6796New |
BTB-1BTB-1 是一种新型的、可逆的选择性 mitotic motor protein Kif18A 抑制剂，其IC50值为1.69 μM。 |
||
| S8439 |
MonastrolMonastrol是一种具有细胞透性的kinesin-5(KIF11)小分子抑制剂，kinesin-5(KIF11)可保持半纺锤体的分离状态。 |
||
| S8215 |
BAY 1217389BAY 1217389一种具有生物口服活性的、选择性丝氨酸/苏氨酸激酶monopolar spindle 1 (Mps1)抑制剂，IC50低于10 nM，具有良好的选择性。 |
||
| S5522 |
H-Cys(Trt)-OHH-Cys(Trt)-OH is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM. |
||
| S7488 |
MPI-0479605MPI-0479605 是一种ATP竞争性的选择性的有丝分裂激酶Mps1抑制剂，IC50为1.8 nM, 其选择性超过其他激酶40倍。 |
||
| S5933 |
K 858K858是一种新型的、有效的Eg5抑制剂，抑制Eg5的ATPase活性，IC50为1.3 μM，对Eg5的选择性是对其他驱动蛋白的至少150倍。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1452 |
Ispinesib (SB-715992)Ispinesib (SB-715992)是一种有效的，特异性的，可逆kinesin spindle protein (KSP)抑制剂，无细胞试验中Kiapp为1.7 nM，对CENP-E， RabK6， MCAK， MKLP1，KHC和Kif1A没有抑制作用。Ispinesib可诱导有丝分裂阻滞和细胞的凋亡。Phase 2。 |
Representative photographs of fluorescent staining of microtubules and nuclei in MDA-MB-231 cells 24 h post-treatment with 4 nM of ispinesib or vinblastine or their combination. Arrows and arrowheads denote mitotic cells with monoploar and bipolar spindles, respectively. Scale bars, 20 um.
|
|
| S2182 |
SB743921 HClSB743921是一种kinesin spindle protein (KSP)（纺锤体驱动蛋白）抑制剂，Ki为0.1 nM，对MKLP1， Kin2， Kif1A， Kif15， KHC， Kif4和CENP-E几乎没有亲和力。Phase 1/2。 |
HeLa cells expressing iRFP were seeded onto 96-well plates and incubated with buffer or different concentrations of SB743921.During the next five days, the plate was scanned with an infrared imaging system (upper panel) to quantify the infrared signals (lower panel). |
|
| S2731 |
AZ 3146AZ 3146是一种选择性Mps1抑制剂，IC50为35 nM左右，有助于聚集CENP-E(驱动蛋白相关的动力蛋白)，对FAK， JNK1， JNK2和Kit作用效果稍弱。 |
Dose response curves for the treatment of breast cancer cell lines in the absence or presence of escalating doses of the TTK inhibitor (TTKi) AZ3146. The survival of cells was measured using the CellTitre MTS/MTA assay carried out 6 days after treatment. Percentage survival (n ¼ 3 per dose) was calculated as the percentage of the signal from treated cells to that from control cells. |
|
| S7090 |
GSK923295GSK923295是一级特异性变构抑制剂CENP-E驱动蛋白ATPase的变构抑制剂，Ki为3.2 nM，对突变型I182和T183作用效果稍弱。Phase 1。 |
(f) HeLa cells were treated with mitotic kinesin CENP-E inhibitor GSK923295 (50 nM) for 1 h to generate misaligned kinetochores. After fixation, cells were stained for ACA, tubulin, and TIP60. Statistical significance was tested by two-sided t-test and represented by asterisks corresponding to ***, p < 0.001. Scale bars, 5 μm. |
|
| S7355 |
ARQ 621ARQ621是一种变构选择性的Eg5 mitotic motor protein抑制剂。第1阶段。 |
||
| S8257New |
CFI-402257CFI-402257 is a potent highly selective, and orally active small-molecule inhibitor of Mps1 with Ki value of 0.09 ± 0.02 nM. |
||
| S6796New |
BTB-1BTB-1 是一种新型的、可逆的选择性 mitotic motor protein Kif18A 抑制剂，其IC50值为1.69 μM。 |
||
| S8439 |
MonastrolMonastrol是一种具有细胞透性的kinesin-5(KIF11)小分子抑制剂，kinesin-5(KIF11)可保持半纺锤体的分离状态。 |
||
| S8215 |
BAY 1217389BAY 1217389一种具有生物口服活性的、选择性丝氨酸/苏氨酸激酶monopolar spindle 1 (Mps1)抑制剂，IC50低于10 nM，具有良好的选择性。 |
||
| S5522 |
H-Cys(Trt)-OHH-Cys(Trt)-OH is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM. |
||
| S7488 |
MPI-0479605MPI-0479605 是一种ATP竞争性的选择性的有丝分裂激酶Mps1抑制剂，IC50为1.8 nM, 其选择性超过其他激酶40倍。 |
||
| S5933 |
K 858K858是一种新型的、有效的Eg5抑制剂，抑制Eg5的ATPase活性，IC50为1.3 μM，对Eg5的选择性是对其他驱动蛋白的至少150倍。 |
沪公网安备 31011502012800号