Kinesin

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抑制剂选择性比较

Kinesin产品

所有产品 Kinesin抑制剂(10)

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K_iapp为1.7 nM，对CENP-E， RabK6， MCAK， MKLP1， KHC和Kif1A没有抑制作用。Phase 2。	Nature, 2019, 575(7781):203-209 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193	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 HCl SB743921是一种kinesin spindle protein (KSP)（纺锤体驱动蛋白）抑制剂，K_i为0.1 nM，对MKLP1， Kin2， Kif1A， Kif15， KHC， Kif4和CENP-E几乎没有亲和力。Phase 1/2。	Mol Cell Proteomics, 2017, 16(3):428-437 Oncotarget, 2017, 8(10):16669-16689 Anticancer Drugs, 2016, 27(9):863-72	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 3146 AZ 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。	Cancer Res, 2019, 79(21):5536-5549 Cell Death Dis, 2019, 10(4):314 Mol Cancer Ther, 2017, 16(11):2552-2562	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	GSK923295 GSK923295是一级特异性变构抑制剂CENP-E驱动蛋白ATPase的变构抑制剂，K_i为3.2 nM，对突变型I182和T183作用效果稍弱。Phase 1。	Nature, 2019, 575(7781):203-209 Cell Syst, 2019, 9(1):74-92.e8 Cancer Res, 2019, 79(21):5536-5549	(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 621 ARQ621是一种变构选择性的Eg5 mitotic motor protein抑制剂。第1阶段。	Mol Cell Proteomics, 2017, 16(3):428-437 Assay Drug Dev Technol, 2016, 14(7):395-406 PLoS One, 2014, 9(9):e105919
S8439	Monastrol Monastrol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。	Nat Commun, 2019, 10(1):175
S8215	BAY 1217389 BAY 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。	Nature, 2019, 575(7781):203-209
S5522	H-Cys(Trt)-OH H-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-0479605 MPI-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。	Curr Biol, 2019, 29(18):3072-3080 Mol Cell Proteomics, 2017, 16(3):428-437
S5933	K 858 K858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K_iapp为1.7 nM，对CENP-E， RabK6， MCAK， MKLP1， KHC和Kif1A没有抑制作用。Phase 2。	Nature,2019, 575(7781):203-209 Cell,2019, 36(2):179-193 Cancer Cell,2019, 36(2):179-193	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 HCl SB743921是一种kinesin spindle protein (KSP)（纺锤体驱动蛋白）抑制剂，K_i为0.1 nM，对MKLP1， Kin2， Kif1A， Kif15， KHC， Kif4和CENP-E几乎没有亲和力。Phase 1/2。	Mol Cell Proteomics,2017, 16(3):428-437 Oncotarget,2017, 8(10):16669-16689 Anticancer Drugs,2016, 27(9):863-72	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 3146 AZ 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。	Cancer Res,2019, 79(21):5536-5549 Cell Death Dis,2019, 10(4):314 Mol Cancer Ther,2017, 16(11):2552-2562	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	GSK923295 GSK923295是一级特异性变构抑制剂CENP-E驱动蛋白ATPase的变构抑制剂，K_i为3.2 nM，对突变型I182和T183作用效果稍弱。Phase 1。	Nature,2019, 575(7781):203-209 Cell Syst,2019, 9(1):74-92.e8 Cancer Res,2019, 79(21):5536-5549	(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 621 ARQ621是一种变构选择性的Eg5 mitotic motor protein抑制剂。第1阶段。	Mol Cell Proteomics,2017, 16(3):428-437 Assay Drug Dev Technol,2016, 14(7):395-406 PLoS One,2014, 9(9):e105919
S8439	Monastrol Monastrol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。	Nat Commun,2019, 10(1):175
S8215	BAY 1217389 BAY 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。	Nature,2019, 575(7781):203-209
S5522	H-Cys(Trt)-OH H-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-0479605 MPI-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。	Curr Biol,2019, 29(18):3072-3080 Mol Cell Proteomics,2017, 16(3):428-437
S5933	K 858 K858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。

Tags: KSP inhibition | Kinesin inhibition | Kinesin assay | Kinesin phosphorylation | Kinesin cancer | KSP inhibitors cancer | KSP inhibitor clinical trial | Kinesin inhibitors list | Kinesin inhibitor review