Microtubule Associated

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S1150	Paclitaxel	<1 mg/mL	171 mg/mL	18 mg/mL
S1148	Docetaxel	<1 mg/mL	100 mg/mL	53 mg/mL
S1241	Vincristine sulfate	60 mg/mL	100 mg/mL	<1 mg/mL
S1364	Patupilone (EPO906, Epothilone B)	<1 mg/mL	102 mg/mL	102 mg/mL
S1165	ABT-751 (E7010)	<1 mg/mL	74 mg/mL	12 mg/mL
S3970	Vindoline	-1 mg/mL	91 mg/mL	-1 mg/mL
S2284	Colchicine	80 mg/mL	80 mg/mL	80 mg/mL
S3725	ELR-510444	<1 mg/mL	73 mg/mL	24 mg/mL
S2775	Nocodazole	<1 mg/mL	7 mg/mL	<1 mg/mL
S3022	Cabazitaxel	<1 mg/mL	100 mg/mL	<1 mg/mL
S2195	Lexibulin (CYT997)	<1 mg/mL	86 mg/mL	20 mg/mL
S1297	Epothilone A	<1 mg/mL	99 mg/mL	99 mg/mL
S7204	Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium	28 mg/mL	<1 mg/mL	<1 mg/mL
S1640	Albendazole	<1 mg/mL	17 mg/mL	<1 mg/mL
S7336	CW069	<1 mg/mL	100 mg/mL	4 mg/mL
S1836	Albendazole Oxide	<1 mg/mL	11 mg/mL	<1 mg/mL
S7721	Monomethyl auristatin E (MMAE)	<1 mg/mL	100 mg/mL	100 mg/mL
S4114	Triclabendazole	<1 mg/mL	72 mg/mL	<1 mg/mL
S7787	Docetaxel Trihydrate	<1 mg/mL	100 mg/mL	100 mg/mL
S7783	Combretastatin A4	<1 mg/mL	63 mg/mL	34 mg/mL
S4071	Griseofulvin	<1 mg/mL	50 mg/mL	<1 mg/mL
S7762	TRx0237 (LMTX) mesylate	95 mg/mL	95 mg/mL	<1 mg/mL
S7497	CK-636	<1 mg/mL	57 mg/mL	50 mg/mL
S4269	Vinorelbine Tartrate	100 mg/mL	100 mg/mL	100 mg/mL
S7495	TAI-1	<1 mg/mL	86 mg/mL	<1 mg/mL
S7930	Ixabepilone (BMS-247550)	<1 mg/mL	100 mg/mL	100 mg/mL
S4505	Vinblastine sulfate	<1 mg/mL	100 mg/mL	<1 mg/mL
S7493	INH1	<1 mg/mL	61 mg/mL	61 mg/mL
S7494	INH6	<1 mg/mL	64 mg/mL	11 mg/mL

Microtubule Associated抑制剂（30）
新Microtubule Associated产品

产品目录	产品描述	文献引用	实验数据
S1150	Paclitaxel Paclitaxel是一种microtubule聚合物稳定剂，在人内皮细胞中IC50为0.1 pM。	Science, 2017, eaal3755 Sci Transl Med, 2018, 10(433) Nat Chem Biol, 2016, 10.1038/nchembio.2082	(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	Docetaxel Docetaxel，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。	Cell, 2018, 174(5):1200-1215 Int J Cancer, 2015, 136(9):2065-77 Oncogenesis, 2014, 3:e100	Viability of cells after exposure to 0, 10, or 10,000 nM docetaxel, assessed by calcein-AM staining (green, left panels) and ethidium homodimer-1 (red, middle panels).
S1241	Vincristine sulfate Vincristine sulfate通过与微管蛋白结合而抑制微管聚合，IC50为32 μM。	Cancer Res, 2013, 73(20):6310-22 J Pharmacol Exp Ther, 2014, 350(3):646-56 Int J Mol Sci, 2012, 13(9):10736-49	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，EC_0.01为1.8 μM。Phase 2。	J Cancer Res Clin Oncol, 2016, 142(11):2281-9 Oncotarget, 2015, 6(13):10893-907 Oncotarget, 2017, 8(2):2694-2707	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。	Bioorg Med Chem, 2013, 21(4):922-31 Fitoterapia, 2017, 116:106-115	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.
S3970^New	Vindoline Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly.
S2254^New	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.
S2284^New	Colchicine Colchicine是一种微管聚合抑制剂， IC50为3 nM。
S3725^New	ELR-510444 ELR-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.
S2775	Nocodazole Nocodazole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。	J Immunol, 2015, 10.4049/jimmunol.1402897 J Biol Chem, 2016, 10.1074/jbc.M116.722751 Cell Signal, 2016, 28(12):1826-1832	A, HeLa cells were treated with DMSO, Taxol (100 nM for 16 h), or Nocodazole (Noco, 100 ng/ml for 16 h). Total cell lysates were probed with the indicated antibodies against Hippo components on Phos-tag SDS-polyacrylamide gels. O and * mark the non-phosphorylated and phosphorylated proteins, respectively.
S3022	Cabazitaxel Cabazitaxel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。	Cell, 2018, 174(5):1200-1215 Mol Cancer Ther, 2017, 10.1158/1535-7163.MCT-17-0179 Oncotarget, 2016, 7(46):76181-76196	ABCB1 functional inhibition using elacridar re-sensitizes TaxR and DU145-DTXR cells to cabazitaxel treatment. A. TaxR and DU145-DTXR cells were subjected to cell growth assays using either vehicle (DMSO), elacridar (0.5μM), cabazitaxel (1nM), or a combination of elacridar and cabazitaxel. Cells were counted 72 hours post-treatment. B. TaxR and DU145-DTXR cells were treated with either vehicle (DMSO), elacridar (0.5μM), cabazitaxel (1nM), or a combination of both elacridar and cabazitaxel for 72 hours. Whole cell lysates were then prepared and subjected to western blot analysis using indicated antibodies. Tubulin served as a loading control. c-PARP = cleaved-PARP, C = control (DMSO) treatment, Elac = elacridar, CTX = cabazitaxel. All data is presented as percent of control mean ± standard deviation. * = p-value ≤ 0.05.
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。	Exp Ther Med, 2013, 6(2):299-304	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 A Epothilone A是一种类似紫杉醇的microtubule（微管）稳定剂，EC_0.01为2 μM。
S7204	Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Fosbretabulin (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K_d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。
S1640	Albendazole Albendazole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	CW069 CW069 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 Oxide Albendazole 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	Triclabendazole Triclabendazole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 Trihydrate Docetaxel，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。	Cell, 2018, 174(5):1200-1215 Int J Cancer, 2015, 136(9):2065-77 Mol Cancer Ther, 2016, 10.1158/1535-7163.MCT-16-0004	(B) Viability of cells after exposure to 0, 10, or 10,000 nM docetaxel, assessed by calcein-AM staining (green, left panels) and ethidium homodimer-1 (red, middle panels). Right panels show merged images. Scale bars = 100 μm.
S7783	Combretastatin A4 Combretastatin A4 是一种以 microtubule 为靶点的试剂，其与β-微管蛋白结合，K_d 为 0.4 μM。Phase 3。
S4071	Griseofulvin Griseofulvin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) mesylate TRx 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-636 CK-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。
S4269	Vinorelbine Tartrate Vinorelbine 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。	Mol Cancer Ther, 2016, 10.1158/1535-7163.MCT-16-0004 PLoS One, 2015, 10(4):e0123901	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-1 TAI-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 sulfate Vinblastine 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	INH1 INH1 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	INH6 INH6 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。

研究领域

产品类型

Microtubule Associated

信号通路图

研究领域