Kinesin

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抑制剂选择性比较

Kinesin产品

所有产品(9) Kinesin抑制剂(9)

目录号	产品描述	文献引用	实验数据
S1452	Ispinesib (SB-715992) Ispinesib (SB-715992, CK0238273)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。Ispinesib可诱导有丝分裂阻滞和细胞的凋亡。Phase 2。	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Sci Transl Med, 2020, 12(562)eaba4434	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。	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Sci Transl Med, 2020, 12(562)eaba4434	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).
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。GSK923295 可诱导有丝分裂后的细胞凋亡。Phase 1。	Cancer Res, 2020, canres.1693.2020 Cancer Res, 2020, 20 pii: canres 883 2019 Cell Rep, 2020, 33(7):108397	(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
S0279^New	Dimethylenastron Dimethylenastron 是一种有效的、特异性的、可逆的 kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) 抑制剂，其IC50值为200 nM。Dimethylenastron 可诱导人多发性骨髓瘤细胞的有丝分裂停滞和凋亡并上调 Hsp70 的表达。
S6796^New	BTB-1 BTB-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	Monastrol 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。	Elife, 2020, 9 Curr Biol, 2020, S0960-9822(20)31673-0 Nat Commun, 2019, 10(1):175
S5522	H-Cys(Trt)-OH H-Cys(Trt)-OH (L-Cys(Trt)-OH, H-L-Cys(Trt)-OH, S-Tritylcysteine) is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM.
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, CK0238273)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。Ispinesib可诱导有丝分裂阻滞和细胞的凋亡。Phase 2。	Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19 Sci Transl Med,2020, 12(562)eaba4434	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。	Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19 Sci Transl Med,2020, 12(562)eaba4434	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).
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。GSK923295 可诱导有丝分裂后的细胞凋亡。Phase 1。	Cancer Res,2020, canres.1693.2020 Cancer Res,2020, 20 pii: canres 883 2019 Cell Rep,2020, 33(7):108397	(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
S0279^New	Dimethylenastron Dimethylenastron 是一种有效的、特异性的、可逆的 kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) 抑制剂，其IC50值为200 nM。Dimethylenastron 可诱导人多发性骨髓瘤细胞的有丝分裂停滞和凋亡并上调 Hsp70 的表达。
S6796^New	BTB-1 BTB-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	Monastrol 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。	Elife,2020, 9 Curr Biol,2020, S0960-9822(20)31673-0 Nat Commun,2019, 10(1):175
S5522	H-Cys(Trt)-OH H-Cys(Trt)-OH (L-Cys(Trt)-OH, H-L-Cys(Trt)-OH, S-Tritylcysteine) is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM.
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