Microtubule Associated
信号通路图
研究领域
抑制剂选择性比较
Microtubule Associated产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1150 |
PaclitaxelPaclitaxel是一种microtubule聚合物稳定剂，在人内皮细胞中IC50为0.1 pM。 |
(F) Kaplan-Meier curves are shown for all groups described: no hydrogel, a hydrogel loaded with paclitaxel, or a hydrogel loaded with doxorubicin. The number of mice per group (n) and median survival (ms) are listed. The experiment was performed at least three times.
|
|
| S1148 |
DocetaxelDocetaxel多西他赛一种taxol类似物，是一种microtubules解聚抑制剂，通过结合于稳定的微管发挥作用。 |
Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
|
|
| S1241 |
Vincristine sulfateVincristine sulfate通过与微管蛋白结合而抑制微管聚合，IC50为32 μM。 |
Plk inhibitor cooperates with chemotherapeutic agents. Conditional patched mutant tumor cells were treated with increasing concentrations of the chemotherapeutic agents vincristine alone or in combination with 10 nMol/L BI-2536. Cells were cultured for 48 hours, pulsed with 3H-Td, and harvested for analysis of 3H-Td incorporation at 66 hours.
|
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| S1364 |
Patupilone (EPO906, Epothilone B)Patupilone (EPO906, Epothilone B)是一种紫杉醇样microtubule稳定剂，EC0.01为1.8 μM。Phase 2。 |
Matrigel invasion assay of H1299 cells treated with SDF-1α or SDF-1α plus Epothilone B prior to 0 or 2 Gy irradiation. After the treatment for 12 h, the H1299 cells that migrated to the bottom surface of the membrane were stained with Giemsa, and the number of migrated cells was calculated manually. |
|
| S1165 |
ABT-751 (E7010)ABT-751 (E7010)与β-tubulin的秋水仙素位点结合，抑制微管的聚合，不抑制MDR转运的底物，且作用于抗Vincristine， Doxorubicin，和Cisplatin的细胞系有效。Phase 1/2。 |
Cell viability in H292 monolayer cells after 3-day treatment and spheroid volume in H292 3D culture
after 7-day treatment with ABT751. Data points are means ?SD for three individual experiments. IC50 values were calculated to emphasize the differences in drug potency in 2D verses 3D cultures. ABT751, IC50 of 177.2 ?17.3 nM for 2D and 670.2 ?257.6 nM for 3D.
|
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| S5919New |
KHS101 hydrochlorideKHS101是TACC3的小分子抑制剂，TACC3是中心体微管动态网络中的关键组分。 |
||
| S8789New |
SSE15206SSE15206是一种微管蛋白聚合抑制剂，在不同来源的癌细胞系中具有抗增殖活性，能克服细胞对靶向微管试剂的抗性。 |
||
| S3970New |
VindolineVindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly. |
||
| S2775 |
NocodazoleNocodazole是一种微管聚合的快速可逆抑制剂，也抑制Abl， Abl(E255K)和Abl(T315I)，IC50分别为0.21 μM， 0.53 μM和0.64 μM。Nocodazole可提高CRISPR介导的同源重组效率，对增强精确的基因编辑效力具有加成作用。 |
AURKA and PRL-3's time-scaled distributions in HCT116 were assessed by synchronization and released after serum starvation (SS) for 24 hours or NOC treatment for 12 hours. Arrows, mitotic cells.
|
|
| S3022 |
CabazitaxelCabazitaxel是一种天然紫杉烷的半合成衍生物，能够抑制细胞分裂和生长，从而杀死癌细胞。抑制微管生长和聚合。 |
Quantification of colony formation assays of aggressive PC cells (DU145-DR and 22Rv1-DR) transfected with control siRNA or two siRNAs targeting each specific nucleoporin following 72 hour treatment with cabazitaxel (25 nM) and single dose radiation (5 Gys).
|
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| S2195 |
Lexibulin (CYT997)Lexibulin (CYT997)作用于癌细胞系，是一种有效的microtubule（微管）聚合抑制剂，IC50为10-100 nM。Phase 2。 |
CYT997 inhibits cellular proliferation in acute myeloid leukemia (AML) cell lines. Cell viability was measured by a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay in 96-well plates in the presence of increasing concentrations of CYT997 for 24 h.The results represent the mean ?SD of four replicates. |
|
| S1297 |
Epothilone AEpothilone A是一种类似紫杉醇的microtubule（微管）稳定剂，EC0.01为2 μM。 |
||
| S7204 |
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) DisodiumFosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium是水溶性的Combretastatin A4 (CA4)前药，CA4靶向作用于microtubule从而与β-微管蛋白结合，无细胞试验中Kd为0.4 μM。Fosbretabulin Disodium抑制微管蛋白聚合，IC50为2.4 μM，也会干扰肿瘤血管。Phase 3。 |
Real-time hemodynamic changes in the tumor upon administration of CA4P. Panel A shows the MRI anatomical reference of the tumor, followed by sO2 maps of a slice of brain showing the largest cross section of the tumor at time points 0, 1, 4 and 6 h. post CA4P administration. Panel B shows the real-time sO2 changes in the tumor and contralateral brain occurring immediately post CA4P administration over 1 hour in a representative animal. SD is represented by lighter shades on the graph. Panel C shows the real-time sO2 changes in the tumor and contralateral brain occurring immediately post CA4P administration (n = 4). Panel D shows the quantification of hypoxia in tumors using CAIX as a marker at times 0 (n = 3), 1 (n = 4) and 6 h. (n = 3) post CA4P administration. Unpaired t-test showed statistically significant difference in CAIX staining at 1 hour post CA4P administration compared to 0 and 6 hours. ** ‐ P > 0.01. Black dotted circle and Red full circle denote the ROIs drawn at the tumor and contralateral brain respectively to compute the sO2.
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| S1640 |
AlbendazoleAlbendazole是一种苯并咪唑类化合物，用于治疗各种蠕虫感染。 |
Dose-dependent disruption in the distribution of α-tubulin following exposure to albendazole. Experimental treatments included vehicle (DMSO), 0.1 μM, 0.5 μM and 1 μM albendazole for 24 hours. α-tubulin was visualized using immunofluorescence (green) and nuclei were stained with DAPI (blue). 40x fluorescence microscopy was used to assess changes in cellular morphology and tubulin distribution.
|
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| S7336 |
CW069CW069 是一种变构选择性microtubule motor protein HSET抑制剂，IC50为75 μM, 其选择性显著高于KSP. |
Spindle morphology before and after addition of the HSET inhibitor (CW069, 200 μM). MTs were visualized by SiR-tubulin staining. Arrowheads indicate split poles. Images were acquired with 5 z-sections (separated by 3 μm) and displayed after maxium projection. Two independent KO lines were analysed (clones #4 and #23). Bar, 5 μm.
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| S1836 |
Albendazole OxideAlbendazole Oxide 是一种微管蛋白聚合或装配抑制剂。 |
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| S7721 |
Monomethyl auristatin E (MMAE)Monomethyl auristatin E (MMAE)是合成的抗肿瘤药，其与单克隆抗体(MAB)有关。它也是一种能够破坏微管的试剂。 |
||
| S4114 |
TriclabendazoleTriclabendazole是一种苯并咪唑类，与微管蛋白结合，损害细胞内运输机制，且干扰蛋白质的合成。 |
||
| S7787 |
Docetaxel TrihydrateDocetaxel，一种紫杉醇类似物，是microtubules解聚抑制剂，通过结合于稳定的微管发挥作用。 |
Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts. Scale bar, 100 μm. Data represent the mean ± SD. *p < 0.05.
|
|
| S2254 |
4-Demethylepipodophyllotoxin(NSC-122819,VM-26)4'-Demethylepipodophyllotoxin is an antimitotic agent which binds to monomeric tubulin, preventing micro-tubule polymerization. It is a potent inhibitor of microtubule assembly. |
||
| S7783 |
Combretastatin A4Combretastatin A4 是一种以 microtubule 为靶点的试剂，其与β-微管蛋白结合，Kd 为 0.4 μM。Phase 3。 |
||
| S2284 |
ColchicineColchicine是一种微管聚合抑制剂， IC50为3 nM。 |
||
| S4071 |
GriseofulvinGriseofulvin是一种灰黄霉菌产物，能够通过干扰微管功能抑制细胞有丝分裂。 |
||
| S7762 |
TRx0237 (LMTX) mesylateTRx 0237 (LMTX™) mesylate是第二代的tau蛋白质聚集抑制剂。用于治疗阿尔茨海默病和额颞痴呆。 |
||
| S7497 |
CK-636CK-636 是一种Arp2/3复合抑制剂，其IC50为4 μM,在24 μM 和 32 μM时，分别能够抑制人的肌动蛋白聚合诱导和裂殖酵母与bovine Arp2/3的复合物。 |
||
| S3725 |
ELR-510444ELR-510444 is a novel microtubule disruptor with potential antivascular effects and in vivo antitumor efficacy, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. |
||
| S4269 |
Vinorelbine TartrateVinorelbine Tartrate是半合成的长春花生物碱，通过与tubulin相互作用抑制有丝分裂。 |
JQ1 and chemotherapeutics (vinorelbine, docetaxel, cisplatin and carboplatin) cooperate to induce apoptosis. MDA-MB-231 and HS578T were exposed to drugs alone and in combination with JQ1, at the indicated doses. Apoptosis was examined after 72 hours of treatment by flow cytometry using Annexin V/ PI staining as previously described.
|
|
| S7495 |
TAI-1TAI-1是一个有效的特异Hec1抑制剂，会打乱Hec1-Nek2蛋白质相互作用。 |
||
| S7930 |
Ixabepilone (BMS-247550)Ixabepilone是一种具有口服活性的微管抑制剂。它与微管蛋白tubulin结合，促进微管蛋白聚合和微管稳定，因此使细胞停留在细胞周期G2-M期，诱导肿瘤细胞的凋亡。 |
||
| S4505 |
Vinblastine sulfateVinblastine sulfate抑制微管形成和nAChR活性，在无细胞实验的测定中，IC50为8.9 μM。 |
||
| S7493 |
INH1INH1 是细胞渗透性的Hec1抑制剂,其特异性地破环Hec1/Nek2相互作用。 |
||
| S7494 |
INH6INH6 是强效的Hec1抑制剂, 其特异性地破坏Hec1/Nek2相互作用，并导致染色体排列异常。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1150 |
PaclitaxelPaclitaxel是一种microtubule聚合物稳定剂，在人内皮细胞中IC50为0.1 pM。 |
(F) Kaplan-Meier curves are shown for all groups described: no hydrogel, a hydrogel loaded with paclitaxel, or a hydrogel loaded with doxorubicin. The number of mice per group (n) and median survival (ms) are listed. The experiment was performed at least three times.
|
|
| S1148 |
DocetaxelDocetaxel多西他赛一种taxol类似物，是一种microtubules解聚抑制剂，通过结合于稳定的微管发挥作用。 |
Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
|
|
| S1241 |
Vincristine sulfateVincristine sulfate通过与微管蛋白结合而抑制微管聚合，IC50为32 μM。 |
Plk inhibitor cooperates with chemotherapeutic agents. Conditional patched mutant tumor cells were treated with increasing concentrations of the chemotherapeutic agents vincristine alone or in combination with 10 nMol/L BI-2536. Cells were cultured for 48 hours, pulsed with 3H-Td, and harvested for analysis of 3H-Td incorporation at 66 hours.
|
|
| S1364 |
Patupilone (EPO906, Epothilone B)Patupilone (EPO906, Epothilone B)是一种紫杉醇样microtubule稳定剂，EC0.01为1.8 μM。Phase 2。 |
Matrigel invasion assay of H1299 cells treated with SDF-1α or SDF-1α plus Epothilone B prior to 0 or 2 Gy irradiation. After the treatment for 12 h, the H1299 cells that migrated to the bottom surface of the membrane were stained with Giemsa, and the number of migrated cells was calculated manually. |
|
| S1165 |
ABT-751 (E7010)ABT-751 (E7010)与β-tubulin的秋水仙素位点结合，抑制微管的聚合，不抑制MDR转运的底物，且作用于抗Vincristine， Doxorubicin，和Cisplatin的细胞系有效。Phase 1/2。 |
Cell viability in H292 monolayer cells after 3-day treatment and spheroid volume in H292 3D culture
after 7-day treatment with ABT751. Data points are means ?SD for three individual experiments. IC50 values were calculated to emphasize the differences in drug potency in 2D verses 3D cultures. ABT751, IC50 of 177.2 ?17.3 nM for 2D and 670.2 ?257.6 nM for 3D.
|
|
| S5919New |
KHS101 hydrochlorideKHS101是TACC3的小分子抑制剂，TACC3是中心体微管动态网络中的关键组分。 |
||
| S8789New |
SSE15206SSE15206是一种微管蛋白聚合抑制剂，在不同来源的癌细胞系中具有抗增殖活性，能克服细胞对靶向微管试剂的抗性。 |
||
| S3970New |
VindolineVindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly. |
||
| S2775 |
NocodazoleNocodazole是一种微管聚合的快速可逆抑制剂，也抑制Abl， Abl(E255K)和Abl(T315I)，IC50分别为0.21 μM， 0.53 μM和0.64 μM。Nocodazole可提高CRISPR介导的同源重组效率，对增强精确的基因编辑效力具有加成作用。 |
AURKA and PRL-3's time-scaled distributions in HCT116 were assessed by synchronization and released after serum starvation (SS) for 24 hours or NOC treatment for 12 hours. Arrows, mitotic cells.
|
|
| S3022 |
CabazitaxelCabazitaxel是一种天然紫杉烷的半合成衍生物，能够抑制细胞分裂和生长，从而杀死癌细胞。抑制微管生长和聚合。 |
Quantification of colony formation assays of aggressive PC cells (DU145-DR and 22Rv1-DR) transfected with control siRNA or two siRNAs targeting each specific nucleoporin following 72 hour treatment with cabazitaxel (25 nM) and single dose radiation (5 Gys).
|
|
| S2195 |
Lexibulin (CYT997)Lexibulin (CYT997)作用于癌细胞系，是一种有效的microtubule（微管）聚合抑制剂，IC50为10-100 nM。Phase 2。 |
CYT997 inhibits cellular proliferation in acute myeloid leukemia (AML) cell lines. Cell viability was measured by a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay in 96-well plates in the presence of increasing concentrations of CYT997 for 24 h.The results represent the mean ?SD of four replicates. |
|
| S1297 |
Epothilone AEpothilone A是一种类似紫杉醇的microtubule（微管）稳定剂，EC0.01为2 μM。 |
||
| S7204 |
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) DisodiumFosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium是水溶性的Combretastatin A4 (CA4)前药，CA4靶向作用于microtubule从而与β-微管蛋白结合，无细胞试验中Kd为0.4 μM。Fosbretabulin Disodium抑制微管蛋白聚合，IC50为2.4 μM，也会干扰肿瘤血管。Phase 3。 |
Real-time hemodynamic changes in the tumor upon administration of CA4P. Panel A shows the MRI anatomical reference of the tumor, followed by sO2 maps of a slice of brain showing the largest cross section of the tumor at time points 0, 1, 4 and 6 h. post CA4P administration. Panel B shows the real-time sO2 changes in the tumor and contralateral brain occurring immediately post CA4P administration over 1 hour in a representative animal. SD is represented by lighter shades on the graph. Panel C shows the real-time sO2 changes in the tumor and contralateral brain occurring immediately post CA4P administration (n = 4). Panel D shows the quantification of hypoxia in tumors using CAIX as a marker at times 0 (n = 3), 1 (n = 4) and 6 h. (n = 3) post CA4P administration. Unpaired t-test showed statistically significant difference in CAIX staining at 1 hour post CA4P administration compared to 0 and 6 hours. ** ‐ P > 0.01. Black dotted circle and Red full circle denote the ROIs drawn at the tumor and contralateral brain respectively to compute the sO2.
|
|
| S1640 |
AlbendazoleAlbendazole是一种苯并咪唑类化合物，用于治疗各种蠕虫感染。 |
Dose-dependent disruption in the distribution of α-tubulin following exposure to albendazole. Experimental treatments included vehicle (DMSO), 0.1 μM, 0.5 μM and 1 μM albendazole for 24 hours. α-tubulin was visualized using immunofluorescence (green) and nuclei were stained with DAPI (blue). 40x fluorescence microscopy was used to assess changes in cellular morphology and tubulin distribution.
|
|
| S7336 |
CW069CW069 是一种变构选择性microtubule motor protein HSET抑制剂，IC50为75 μM, 其选择性显著高于KSP. |
Spindle morphology before and after addition of the HSET inhibitor (CW069, 200 μM). MTs were visualized by SiR-tubulin staining. Arrowheads indicate split poles. Images were acquired with 5 z-sections (separated by 3 μm) and displayed after maxium projection. Two independent KO lines were analysed (clones #4 and #23). Bar, 5 μm.
|
|
| S1836 |
Albendazole OxideAlbendazole Oxide 是一种微管蛋白聚合或装配抑制剂。 |
||
| S7721 |
Monomethyl auristatin E (MMAE)Monomethyl auristatin E (MMAE)是合成的抗肿瘤药，其与单克隆抗体(MAB)有关。它也是一种能够破坏微管的试剂。 |
||
| S4114 |
TriclabendazoleTriclabendazole是一种苯并咪唑类，与微管蛋白结合，损害细胞内运输机制，且干扰蛋白质的合成。 |
||
| S7787 |
Docetaxel TrihydrateDocetaxel，一种紫杉醇类似物，是microtubules解聚抑制剂，通过结合于稳定的微管发挥作用。 |
Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts. Scale bar, 100 μm. Data represent the mean ± SD. *p < 0.05.
|
|
| S2254 |
4-Demethylepipodophyllotoxin(NSC-122819,VM-26)4'-Demethylepipodophyllotoxin is an antimitotic agent which binds to monomeric tubulin, preventing micro-tubule polymerization. It is a potent inhibitor of microtubule assembly. |
||
| S7783 |
Combretastatin A4Combretastatin A4 是一种以 microtubule 为靶点的试剂，其与β-微管蛋白结合，Kd 为 0.4 μM。Phase 3。 |
||
| S2284 |
ColchicineColchicine是一种微管聚合抑制剂， IC50为3 nM。 |
||
| S4071 |
GriseofulvinGriseofulvin是一种灰黄霉菌产物，能够通过干扰微管功能抑制细胞有丝分裂。 |
||
| S7762 |
TRx0237 (LMTX) mesylateTRx 0237 (LMTX™) mesylate是第二代的tau蛋白质聚集抑制剂。用于治疗阿尔茨海默病和额颞痴呆。 |
||
| S7497 |
CK-636CK-636 是一种Arp2/3复合抑制剂，其IC50为4 μM,在24 μM 和 32 μM时，分别能够抑制人的肌动蛋白聚合诱导和裂殖酵母与bovine Arp2/3的复合物。 |
||
| S3725 |
ELR-510444ELR-510444 is a novel microtubule disruptor with potential antivascular effects and in vivo antitumor efficacy, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. |
||
| S4269 |
Vinorelbine TartrateVinorelbine Tartrate是半合成的长春花生物碱，通过与tubulin相互作用抑制有丝分裂。 |
JQ1 and chemotherapeutics (vinorelbine, docetaxel, cisplatin and carboplatin) cooperate to induce apoptosis. MDA-MB-231 and HS578T were exposed to drugs alone and in combination with JQ1, at the indicated doses. Apoptosis was examined after 72 hours of treatment by flow cytometry using Annexin V/ PI staining as previously described.
|
|
| S7495 |
TAI-1TAI-1是一个有效的特异Hec1抑制剂，会打乱Hec1-Nek2蛋白质相互作用。 |
||
| S7930 |
Ixabepilone (BMS-247550)Ixabepilone是一种具有口服活性的微管抑制剂。它与微管蛋白tubulin结合，促进微管蛋白聚合和微管稳定，因此使细胞停留在细胞周期G2-M期，诱导肿瘤细胞的凋亡。 |
||
| S4505 |
Vinblastine sulfateVinblastine sulfate抑制微管形成和nAChR活性，在无细胞实验的测定中，IC50为8.9 μM。 |
||
| S7493 |
INH1INH1 是细胞渗透性的Hec1抑制剂,其特异性地破环Hec1/Nek2相互作用。 |
||
| S7494 |
INH6INH6 是强效的Hec1抑制剂, 其特异性地破坏Hec1/Nek2相互作用，并导致染色体排列异常。 |
