微小管関連

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
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 (Epothilone B)	<1 mg/mL	102 mg/mL	102 mg/mL
S3220	Trigonelline	-1 mg/mL	50 mg/mL	-1 mg/mL
S3206	5a-Pregnane-3,20-dione	<1 mg/mL	3 mg/mL	3.5 mg/mL
S0444	Indibulin	<1 mg/mL	40 mg/mL	<1 mg/mL
S0328	MMAF	100 mg/mL	100 mg/mL	100 mg/mL
S0360	EGFR Inhibitor	˂1 mg/mL	83 mg/mL	2 mg/mL
S2441	Estramustine phosphate sodium	100 mg/mL	<1 mg/mL	<1 mg/mL
S2444	Parbendazole	<1 mg/mL	3 mg/mL	<1 mg/mL
S6661	VcMMAE	<1 mg/mL	100 mg/mL	100 mg/mL
S1165	ABT-751 (E7010)	<1 mg/mL	74 mg/mL	12 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
S3970	Vindoline	-1 mg/mL	91 mg/mL	-1 mg/mL
S8789	SSE15206	<1 mg/mL	74 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
S2284	Colchicine	80 mg/mL	80 mg/mL	80 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
S3725	ELR-510444	<1 mg/mL	73 mg/mL	24 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
S4535	Methylene Blue	63 mg/mL	63 mg/mL	'10 mg/mL
S5919	KHS101 hydrochloride	3 mg/mL	75 mg/mL	57 mg/mL
S1233	2-Methoxyestradiol (2-MeOE2)	<1 mg/mL	60 mg/mL	<1 mg/mL
S1176	Plinabulin (NPI-2358)	<1 mg/mL	54 mg/mL	<1 mg/mL

Microtubule Associated製品

All (45) Microtubule Associated阻害剤(43) Microtubule Associatedモジュレータ(2)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1150	Paclitaxel Paclitaxel (NSC 125973, PTX, Taxol, Onxal) is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.	Cancer Cell, 2020, 38(5):672-684.e6 Clin Cancer Res, 2020, 27 pii: clincanres J Cell Biol, 2020, 4;219(5):e201909094	Microscope image (406) magnification of U937 cells after exposure to SM-TNs. a) Untreated U937 cells. b) U937 cells treated with 200 nM, and 35 nM ODS empty shells. c) U937 cells treated with microcrystalline (free) Taxol prepared by sonicating Taxol in 20%H3PO4/0.8% SDS solution. d) U937 cells treated with 200 nM SM-TN. A SM-TN is seen in the middle of the picture. e) U937 cells treated with 35 nM SMTN.The nanowires are too small to see at this magnification, but their effect on the cells is clearly visible. Scale bar = 10 mm.
S1148	Docetaxel Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.	Mol Med Rep, 2021, 23(1)40 Nat Commun, 2020, 10;11(1):2935 J Immunother Cancer, 2020, 8(2)e000807
S1241	Vincristine sulfate Vincristine sulfate (Leurocristine) is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.	Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-20-1315 Oncogene, 2020, 39(17):3555-3570 Environ Sci Technol, 2020, 54(23):15267-15276	for HXO-RB44 cells, IC50 values for VCR were changed in the different SG600 treatment groups. The results are representative of three independent experiments and of f our replicates in each experiment.
S1364	Patupilone (Epothilone B) Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC_0.01 of 1.8 μM. Phase 2.	Cancer Res, 2020, canres.530.2020 Front Immunol, 2019, 10:72 Sci Rep, 2019, 9(1):19384	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.
S3220^新	Trigonelline Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells.
S3206^新	5a-Pregnane-3,20-dione 5a-Pregnane-3,20-dione (5alphaP, 5-a-dihydroprogesterone, 3,20-allopregnanedione, 5-Alpha-Dihydro Progesterone) is the endogenous progesterone metabolite. 5a-Pregnane-3,20-dione depolymerizes actin and decreases expression of actin and vinculin. 5a-Pregnane-3,20-dione is involved in promoting breast neoplasia and metastasis by affecting adhesion and cytoskeletal molecules.
S2440^新	Vindesine sulfate Vindesine sulfate (Eldesine, Eldisine, Desacetyl Vinblastine amide, Desacetylvinblastine amide, DAVA, DVA, VDS), a vinca alkaloid derived from Catharanthus roseus, is a potent inhibitor of mitosis with antineoplastic activities. Vindesine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.	Sci Rep, 2020, 10(1):13124
S0444^新	Indibulin Indibulin (ZIO 301, D 24851, Zybulin) is an orally applied inhibitor of tubulin assembly with potent anticancer activity. Indibulin induces mitotic arrest and apoptosis.	Bioorg Med Chem, 2020, 28(20):115712
S0328^新	MMAF MMAF (Monomethylauristatin F) is a synthetic antineoplastic agent and a potent inhibitor of tubulin polymerization. MMAF (Monomethylauristatin F) is applied as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin, ABT-414 and SGN-CD19A.
S0360^新	EGFR Inhibitor EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.
S2441^新	Estramustine phosphate sodium Estramustine phosphate sodium is an antitumour drug with a unique dual mode of action. Estrone and estradiol, products of the metabolism of estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels. Estramustine(the cytotoxic metabolite produced by dephosphorylation of estramustine phosphate sodium) is an antiprostatic tumor drug with antimicrotubule effects.
S2444^新	Parbendazole Parbendazole is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules.
S6661^新	VcMMAE VcMMAE (mc-vc-PAB-MMAE), a MMAE derivative with valine-citrulline (Vc) linker, is an antibody-drug conjugate (ADC) with potent antitumor activity. MMAE is a synthetic antineoplastic agent and can be efficiently released from VcMMAE in vitro and exert cytotoxic activity.
S6765^新	MMAD MMAD (Demethyldolastatin 10, Monomethylauristatin D, Monomethyl Dolastatin 10) is a highly toxic inhibitor of tubulin.
S1165	ABT-751 (E7010) ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.	J Clin Invest, 2020, 10.1172/JCI122462 Fitoterapia, 2017, 116:106-115 PLoS Genet, 2016, 12(9):e1006279	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.
S2775	Nocodazole Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.	Cell, 2020, 19;180(6):1198-1211.e19. Cell, 2020, 19;180(6):1198-1211e19 Nat Methods, 2020, 17(3):279-282	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 (RPR-116258A, XRP6258, TXD 258) is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.	Cells, 2020, 28;9(5) Cells, 2020, 9(1) Mol Cancer Ther, 2020, 19(2):364-374	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, SRI-32007) is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. Phase 2.	Adv Virol, 2020, 2020:8844061 J Exp Clin Cancer Res, 2019, 38(1):44 J Cell Mol Med, 2019, 23(2):1174-1182	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 is a paclitaxel-like microtubule-stabilizing agent with EC_0.01 of 2 μM.	Cancers (Basel), 2020, 12(12)E3816 Sci Rep, 2020, 10(1):13124 Toxicol Sci, 2019, 10.1093/toxsci/kfz123
S7204	Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with K_d of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Fosbretabulin disodium induces mitotic arrest and apoptosis in endothelial cells. Phase 3.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 J Drug Target, 2020, 10.1080/1061186X.2020.1818759	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	Albendazole Albendazole (SKF-62979) is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.	Mol Cancer Ther, 2020, molcanther.0525.2020 Sci Rep, 2020, 10(1):13124 Cell Death Dis, 2020, 11(8):684	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 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over KSP.	EMBO Rep, 2020, 9:e49234 Mol Syst Biol, 2018, 14(8):e8238 Anticancer Res, 2018, 38(6):3393-3400	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 (Ricobendazole) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.
S7721	Monomethyl auristatin E (MMAE) Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent, which is linked to a monoclonal antibody (MAB). It is also a microtubule-disrupting agent .	Cancer Lett, 2017, 409:125-136 Oncotarget, 2017,
S4114	Triclabendazole Triclabendazole (CGA-89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.
S3970	Vindoline Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly.	Nat Commun, 2020, 11(1):941
S8789	SSE15206 SSE15206 is a tubulin polymerization inhibitor that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents.
S7787	Docetaxel Trihydrate Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.	Mol Med Rep, 2021, 23(1)40 Am J Cancer Res, 2020, 10(10):3302-3315 Front Oncol, 2020, 10:524922	(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.
S2254	4-Demethylepipodophyllotoxin(NSC-122819,VM-26) 4-Demethylepipodophyllotoxin (NSC-122819, VM-26, DMEP) is an antimitotic agent which binds to monomeric tubulin, preventing micro-tubule polymerization. It is a potent inhibitor of microtubule assembly.	Front Pharmacol, 2019, 10:381
S7783	Combretastatin A4 Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with K_d of 0.4 μM.Phase 3.	Mol Cancer Ther, 2020, molcanther.0525.2020 Mol Pharmacol, 2019, 96(6):711-719 Drug Des Devel Ther, 2017, 11:1335-1351
S2284	Colchicine Colchicine (Colchineos, Colchisol, Colcin) is a microtubule polymerization inhibitor with an IC50 of 3 nM.	Cell Rep, 2020, 31(12):107794 Am J Cancer Res, 2020, 10(8):2649-2676 J Biol Chem, 2019, 294(20):8161-8170
S4071	Griseofulvin Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.
S7762	TRx0237 (LMTX) mesylate TRx 0237 (LMTX) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.
S7497	CK-636 CK-636 (CK-0944636) is an Arp2/3 complex inhibitor with IC50 of 4 μM, 24 μM and 32 μM for inhibition of actin polymerization induced by human, fission yeast and bovine Arp2/3 complex, respectively.	Theranostics, 2019, 9(25):7628-7647 Front Cell Infect Microbiol, 2017, 7:400 Oncotarget, 2017, 8(20):33353-33364
S3725	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.
S4269	Vinorelbine Tartrate Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.	Int J Mol Sci, 2020, 21(23)E9034 Cancer Chemother Pharmacol, 2020, 86(6):841-846 Sci Rep, 2020, 10(1):13124	Activity of vinorelbine in NSCLC cell lines in cell viability assay. Activity of vinorelbine NCI-H23, NCI-H460, and NCC44 cell lines in a Cell Titer Glo cell viability assay. Cells were treated with increasing drug concentrations from 0-10000 nM. The data are plotted as the mean % of control cells against the corresponding drug concentration.
S7495	TAI-1 TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.	J Exp Clin Cancer Res, 2019, 18;38(1):316 Curr Biol, 2019, 29(18):3072-3080
S7930	Ixabepilone (BMS-247550) Ixabepilone (BMS-247550, Azaepothilone B, BMS 247550-1, Ixempra) is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S4505	Vinblastine sulfate Vinblastine sulfate (NSC49842) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.	Mol Cancer Ther, 2020, 25;molcanther.1021.2019 Mutagenesis, 2020, 10.1093/mutage/geaa003 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S7493	INH1 INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.	J Clin Invest, 2018, 128(7):2877-2893
S7494	INH6 INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
S4535	Methylene Blue Methylene Blue (Basic Blue 9, Tetramethylthionine chloride, methylthioninium chloride, CI-52015) is used as a dye in chromoendoscopy. It Inhibits tau filament formation with IC50 of 1.9μM. Also it inhibits soluble guanylyl cyclase.	bioRxiv, 2020, 2020/9/20.4.7.30734
S5919	KHS101 hydrochloride KHS101 is a small-molecule inhibitor of TACC3, which is a key component of centrosome-microtubule dynamic networks.
S1233	2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.	J Cell Mol Med, 2020, 10.1111/jcmm.15892 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Pancreatic cancer cell lines (CFPAC-1 and BxPC-3) were treated with siHIF-1 and 2-ME and then evaluate the expression HIF-1α, CRT and P-eIF2α by Western blotting experiment.
S1176	Plinabulin (NPI-2358) Plinabulin (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. Phase 1/2.	J Biol Chem, 2019, 294(20):8161-8170 Mol Pharmacol, 2019, 96(6):711-719 Curr Protoc Chem Biol, 2013, 5(3):195-212

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1150	Paclitaxel Paclitaxel (NSC 125973, PTX, Taxol, Onxal) is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.	Cancer Cell, 2020, 38(5):672-684.e6 Clin Cancer Res, 2020, 27 pii: clincanres J Cell Biol, 2020, 4;219(5):e201909094	Microscope image (406) magnification of U937 cells after exposure to SM-TNs. a) Untreated U937 cells. b) U937 cells treated with 200 nM, and 35 nM ODS empty shells. c) U937 cells treated with microcrystalline (free) Taxol prepared by sonicating Taxol in 20%H3PO4/0.8% SDS solution. d) U937 cells treated with 200 nM SM-TN. A SM-TN is seen in the middle of the picture. e) U937 cells treated with 35 nM SMTN.The nanowires are too small to see at this magnification, but their effect on the cells is clearly visible. Scale bar = 10 mm.
S1148	Docetaxel Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.	Mol Med Rep, 2021, 23(1)40 Nat Commun, 2020, 10;11(1):2935 J Immunother Cancer, 2020, 8(2)e000807
S1241	Vincristine sulfate Vincristine sulfate (Leurocristine) is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.	Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-20-1315 Oncogene, 2020, 39(17):3555-3570 Environ Sci Technol, 2020, 54(23):15267-15276	for HXO-RB44 cells, IC50 values for VCR were changed in the different SG600 treatment groups. The results are representative of three independent experiments and of f our replicates in each experiment.
S1364	Patupilone (Epothilone B) Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC_0.01 of 1.8 μM. Phase 2.	Cancer Res, 2020, canres.530.2020 Front Immunol, 2019, 10:72 Sci Rep, 2019, 9(1):19384	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.
S3220^新	Trigonelline Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells.
S3206^新	5a-Pregnane-3,20-dione 5a-Pregnane-3,20-dione (5alphaP, 5-a-dihydroprogesterone, 3,20-allopregnanedione, 5-Alpha-Dihydro Progesterone) is the endogenous progesterone metabolite. 5a-Pregnane-3,20-dione depolymerizes actin and decreases expression of actin and vinculin. 5a-Pregnane-3,20-dione is involved in promoting breast neoplasia and metastasis by affecting adhesion and cytoskeletal molecules.
S2440^新	Vindesine sulfate Vindesine sulfate (Eldesine, Eldisine, Desacetyl Vinblastine amide, Desacetylvinblastine amide, DAVA, DVA, VDS), a vinca alkaloid derived from Catharanthus roseus, is a potent inhibitor of mitosis with antineoplastic activities. Vindesine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.	Sci Rep, 2020, 10(1):13124
S0444^新	Indibulin Indibulin (ZIO 301, D 24851, Zybulin) is an orally applied inhibitor of tubulin assembly with potent anticancer activity. Indibulin induces mitotic arrest and apoptosis.	Bioorg Med Chem, 2020, 28(20):115712
S0328^新	MMAF MMAF (Monomethylauristatin F) is a synthetic antineoplastic agent and a potent inhibitor of tubulin polymerization. MMAF (Monomethylauristatin F) is applied as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin, ABT-414 and SGN-CD19A.
S0360^新	EGFR Inhibitor EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.
S2441^新	Estramustine phosphate sodium Estramustine phosphate sodium is an antitumour drug with a unique dual mode of action. Estrone and estradiol, products of the metabolism of estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels. Estramustine(the cytotoxic metabolite produced by dephosphorylation of estramustine phosphate sodium) is an antiprostatic tumor drug with antimicrotubule effects.
S2444^新	Parbendazole Parbendazole is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules.
S6661^新	VcMMAE VcMMAE (mc-vc-PAB-MMAE), a MMAE derivative with valine-citrulline (Vc) linker, is an antibody-drug conjugate (ADC) with potent antitumor activity. MMAE is a synthetic antineoplastic agent and can be efficiently released from VcMMAE in vitro and exert cytotoxic activity.
S6765^新	MMAD MMAD (Demethyldolastatin 10, Monomethylauristatin D, Monomethyl Dolastatin 10) is a highly toxic inhibitor of tubulin.
S1165	ABT-751 (E7010) ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.	J Clin Invest, 2020, 10.1172/JCI122462 Fitoterapia, 2017, 116:106-115 PLoS Genet, 2016, 12(9):e1006279	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.
S2775	Nocodazole Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.	Cell, 2020, 19;180(6):1198-1211.e19. Cell, 2020, 19;180(6):1198-1211e19 Nat Methods, 2020, 17(3):279-282	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 (RPR-116258A, XRP6258, TXD 258) is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.	Cells, 2020, 28;9(5) Cells, 2020, 9(1) Mol Cancer Ther, 2020, 19(2):364-374	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, SRI-32007) is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. Phase 2.	Adv Virol, 2020, 2020:8844061 J Exp Clin Cancer Res, 2019, 38(1):44 J Cell Mol Med, 2019, 23(2):1174-1182	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 is a paclitaxel-like microtubule-stabilizing agent with EC_0.01 of 2 μM.	Cancers (Basel), 2020, 12(12)E3816 Sci Rep, 2020, 10(1):13124 Toxicol Sci, 2019, 10.1093/toxsci/kfz123
S7204	Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with K_d of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Fosbretabulin disodium induces mitotic arrest and apoptosis in endothelial cells. Phase 3.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 J Drug Target, 2020, 10.1080/1061186X.2020.1818759	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	Albendazole Albendazole (SKF-62979) is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.	Mol Cancer Ther, 2020, molcanther.0525.2020 Sci Rep, 2020, 10(1):13124 Cell Death Dis, 2020, 11(8):684	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 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over KSP.	EMBO Rep, 2020, 9:e49234 Mol Syst Biol, 2018, 14(8):e8238 Anticancer Res, 2018, 38(6):3393-3400	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 (Ricobendazole) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.
S7721	Monomethyl auristatin E (MMAE) Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent, which is linked to a monoclonal antibody (MAB). It is also a microtubule-disrupting agent .	Cancer Lett, 2017, 409:125-136 Oncotarget, 2017,
S4114	Triclabendazole Triclabendazole (CGA-89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.
S3970	Vindoline Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly.	Nat Commun, 2020, 11(1):941
S8789	SSE15206 SSE15206 is a tubulin polymerization inhibitor that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents.
S7787	Docetaxel Trihydrate Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.	Mol Med Rep, 2021, 23(1)40 Am J Cancer Res, 2020, 10(10):3302-3315 Front Oncol, 2020, 10:524922	(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.
S2254	4-Demethylepipodophyllotoxin(NSC-122819,VM-26) 4-Demethylepipodophyllotoxin (NSC-122819, VM-26, DMEP) is an antimitotic agent which binds to monomeric tubulin, preventing micro-tubule polymerization. It is a potent inhibitor of microtubule assembly.	Front Pharmacol, 2019, 10:381
S7783	Combretastatin A4 Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with K_d of 0.4 μM.Phase 3.	Mol Cancer Ther, 2020, molcanther.0525.2020 Mol Pharmacol, 2019, 96(6):711-719 Drug Des Devel Ther, 2017, 11:1335-1351
S2284	Colchicine Colchicine (Colchineos, Colchisol, Colcin) is a microtubule polymerization inhibitor with an IC50 of 3 nM.	Cell Rep, 2020, 31(12):107794 Am J Cancer Res, 2020, 10(8):2649-2676 J Biol Chem, 2019, 294(20):8161-8170
S4071	Griseofulvin Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.
S7762	TRx0237 (LMTX) mesylate TRx 0237 (LMTX) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.
S7497	CK-636 CK-636 (CK-0944636) is an Arp2/3 complex inhibitor with IC50 of 4 μM, 24 μM and 32 μM for inhibition of actin polymerization induced by human, fission yeast and bovine Arp2/3 complex, respectively.	Theranostics, 2019, 9(25):7628-7647 Front Cell Infect Microbiol, 2017, 7:400 Oncotarget, 2017, 8(20):33353-33364
S3725	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.
S4269	Vinorelbine Tartrate Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.	Int J Mol Sci, 2020, 21(23)E9034 Cancer Chemother Pharmacol, 2020, 86(6):841-846 Sci Rep, 2020, 10(1):13124	Activity of vinorelbine in NSCLC cell lines in cell viability assay. Activity of vinorelbine NCI-H23, NCI-H460, and NCC44 cell lines in a Cell Titer Glo cell viability assay. Cells were treated with increasing drug concentrations from 0-10000 nM. The data are plotted as the mean % of control cells against the corresponding drug concentration.
S7495	TAI-1 TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.	J Exp Clin Cancer Res, 2019, 18;38(1):316 Curr Biol, 2019, 29(18):3072-3080
S7930	Ixabepilone (BMS-247550) Ixabepilone (BMS-247550, Azaepothilone B, BMS 247550-1, Ixempra) is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S4505	Vinblastine sulfate Vinblastine sulfate (NSC49842) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.	Mol Cancer Ther, 2020, 25;molcanther.1021.2019 Mutagenesis, 2020, 10.1093/mutage/geaa003 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S7493	INH1 INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.	J Clin Invest, 2018, 128(7):2877-2893
S7494	INH6 INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
S4535	Methylene Blue Methylene Blue (Basic Blue 9, Tetramethylthionine chloride, methylthioninium chloride, CI-52015) is used as a dye in chromoendoscopy. It Inhibits tau filament formation with IC50 of 1.9μM. Also it inhibits soluble guanylyl cyclase.	bioRxiv, 2020, 2020/9/20.4.7.30734
S5919	KHS101 hydrochloride KHS101 is a small-molecule inhibitor of TACC3, which is a key component of centrosome-microtubule dynamic networks.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1233	2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.	J Cell Mol Med, 2020, 10.1111/jcmm.15892 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Pancreatic cancer cell lines (CFPAC-1 and BxPC-3) were treated with siHIF-1 and 2-ME and then evaluate the expression HIF-1α, CRT and P-eIF2α by Western blotting experiment.
S1176	Plinabulin (NPI-2358) Plinabulin (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. Phase 1/2.	J Biol Chem, 2019, 294(20):8161-8170 Mol Pharmacol, 2019, 96(6):711-719 Curr Protoc Chem Biol, 2013, 5(3):195-212

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文献中Selleckの製品使用例

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S1233

2-Methoxyestradiol (2-MeOE2)

2-Methoxyestradiol (2-MeOE2, NSC 659853) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.

J Cell Mol Med, 2020, 10.1111/jcmm.15892

Cancer Cell Int, 2020, 19;20:58

Hum Cell, 2020, 10.1007/s13577-020-00420-z