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) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1150 | Paclitaxel (NSC 125973) | <1 mg/mL | 171 mg/mL | ''18 mg/mL |
| S1148 | Docetaxel (RP56976) | <1 mg/mL | 100 mg/mL | '53 mg/mL |
| S1241 | Vincristine (NSC-67574) sulfate | 60 mg/mL | 100 mg/mL | '''<1 mg/mL |
| S1364 | Patupilone (Epothilone B) | <1 mg/mL | 102 mg/mL | 102 mg/mL |
| E2402 | T-1101 tosylate | <1 mg/mL | 100 mg/mL | 3 mg/mL |
| S8912 | Eribulin Mesylate (E7389) | ' mg/mL | ||
| S6954 | CK-869 | <1 mg/mL | 79 mg/mL | '''<1 mg/mL |
| S1165 | ABT-751 (E7010) | <1 mg/mL | 74 mg/mL | 12 mg/mL |
| S2775 | Nocodazole (R17934) | <1 mg/mL | 7 mg/mL | ''<1 mg/mL |
| S3022 | Cabazitaxel (XRP6258) | <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 (SKF-62979) | <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 |
| S5256 | Benproperine phosphate | 81 mg/mL | 60 mg/mL | '''3 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 |
| S0328 | MMAF | 100 mg/mL | 100 mg/mL | 100 mg/mL |
| S2284 | Colchicine (NSC 757) | 80 mg/mL | 80 mg/mL | '80 mg/mL |
| S2447 | Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222) | <1 mg/mL | 100 mg/mL | 55 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 ditartrate (KW-2307) | 100 mg/mL | 100 mg/mL | ''100 mg/mL |
| S6661 | VcMMAE | <1 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 (NSC-49842) sulfate | <1 mg/mL | 100 mg/mL | ''''<1 mg/mL |
| S7493 | INH1 | <1 mg/mL | 61 mg/mL | '61 mg/mL |
| S6773 | Mertansine | <1 mg/mL | 50 mg/mL | '''2 mg/mL |
| S7494 | INH6 | <1 mg/mL | 64 mg/mL | 11 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 |
| S4535 | Methylene Blue | 63 mg/mL | 63 mg/mL | '10 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 |
| S3220 | Trigonelline | -1 mg/mL | 50 mg/mL | -1 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 |
| S3374 | Verubulin hydrochloride | 56 mg/mL | 56 mg/mL | 56 mg/mL |
| S0360 | EGFR Inhibitor | ˂1 mg/mL | 83 mg/mL | 2 mg/mL |
Microtubule Associated製品
| 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 (NSC 125973)Paclitaxel (NSC 125973, PTX, Taxol, Onxal, Abraxane) is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells. |
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 (RP56976)Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
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| S1241 |
Vincristine (NSC-67574) sulfateVincristine sulfate (NSC-67574, Leurocristine, Oncovin, 22-Oxovincaleukoblastine) 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. |
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 EC0.01 of 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. |
|
| E2402新 |
T-1101 tosylateT-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. |
||
| S8912新 |
Eribulin Mesylate (E7389)Eribulin Mesylate (E7389, B-1939, ER-086526), an analogue of the marine natural product halichondrin B, is a nontaxane completely synthetic microtubule inhibitor. |
||
| S6954新 |
CK-869CK-869 (CK 0157869) is a small molecule inhibitor of actin-related protein 2/3 (Arp2/3) complex with an IC50 of 7 μM. CK-869 can directly suppresses microtubule assembly both in vitro and in vivo. |
||
| 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. |
Cell viability in H292 monolayer cells after 3-day treatment and spheroid volume in H292 3D cultureafter 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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| S2775 |
Nocodazole (R17934)Nocodazole (R17934, Oncodazole, NSC238159) 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. |
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. |
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| S3022 |
Cabazitaxel (XRP6258)Cabazitaxel (RPR-116258A, XRP6258, TXD 258, Taxoid XRP6258) 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. |
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. |
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| 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. |
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. |
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| S1297 |
Epothilone AEpothilone A is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 2 μM. |
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| S7204 |
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) DisodiumFosbretabulin (Combretastatin A4 Phosphate, CA4P, CA 4DP) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd 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. |
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 |
Albendazole (SKF-62979)Albendazole (SKF-62979) is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations. |
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 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over 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 (Ricobendazole) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations. |
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| S2440 |
Vindesine sulfateVindesine 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. |
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| S5256 |
Benproperine phosphateBenproperine phosphate (Blascorid, Pirexyl), a cough suppressant, is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate suppresses cancer cell migration and tumor metastasis. |
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| S7721 |
Monomethyl auristatin E (MMAE)Monomethyl auristatin E (MMAE, SGD-1010) is a synthetic antineoplastic agent, which is linked to a monoclonal antibody (MAB). It is also a microtubule-disrupting agent . |
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| S4114 |
TriclabendazoleTriclabendazole (CGA-89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis. |
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| S3970 |
VindolineVindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly. |
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| S8789 |
SSE15206SSE15206 is a tubulin polymerization inhibitor that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents. |
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| S7787 |
Docetaxel TrihydrateDocetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
(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. |
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| 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. |
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| S7783 |
Combretastatin A4Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3. |
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| S0328 |
MMAFMMAF (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. |
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| S2284 |
Colchicine (NSC 757)Colchicine (NSC 757, Colchineos, Colchisol, Colcin) is a microtubule polymerization inhibitor with an IC50 of 3 nM. |
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| S2447 |
Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222)Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222, Antibiotic C 15003P3) is a potent inhibitor of tubulin polymerization with IC50 of 3.4 μM. |
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| S4071 |
GriseofulvinGriseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function. |
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| S7762 |
TRx0237 (LMTX) mesylateTRx 0237 mesylate (LMTX, Hydromethylthionine) is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia. |
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| S7497 |
CK-636CK-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. |
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| 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. |
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| S4269 |
Vinorelbine ditartrate (KW-2307)Vinorelbine Tartrate (KW-2307, Nor-5'-anhydrovinblastine ditartrate) 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. |
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.
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| S6661 |
VcMMAEVcMMAE (mc-vc-PAB-MMAE), a MMAE derivative with valine-citrulline (Vc) linker,is an Drug-linker Conjugate for 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. |
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| S7495 |
TAI-1TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction. |
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| S7930 |
Ixabepilone (BMS-247550)Ixabepilone (BMS-247550, Azaepothilone B, BMS 247550-1, Ixempra, Aza-epothilone B) 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. |
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| S4505 |
Vinblastine (NSC-49842) sulfateVinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) 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. |
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| S7493 |
INH1INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction. |
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| S6773 |
MertansineMertansine (DM1, Maytansinoid DM1), an antibody-conjugatable maytansinoid, is a selective microtubule inhibitor that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC). Solutions are best fresh-prepared. |
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| S7494 |
INH6INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment. |
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| S3206 |
5a-Pregnane-3,20-dione5a-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. |
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| S0444 |
IndibulinIndibulin (ZIO 301, D 24851, Zybulin) is an orally applied inhibitor of tubulin assembly with potent anticancer activity. Indibulin induces mitotic arrest and apoptosis. |
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| S4535 |
Methylene BlueMethylene 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. |
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| S2441 |
Estramustine phosphate sodiumEstramustine phosphate sodium (EMP, Emcyt, Estracyt) 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. |
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| S2444 |
ParbendazoleParbendazole (SKF 29044) is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules. |
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| S9555 |
VincristineVincristine (Leurocristine, NSC-67574, 22-Oxovincaleukoblastine) is a natural alkaloid isolated from the plant Vinca rosea Linn. with anti-tumor activity. Vincristine inhibits microtubule formation in mitotic spindle and binds to microtubule with Ki of 85 nM. |
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| S3220 |
TrigonellineTrigonelline (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. |
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| S5919 |
KHS101 hydrochlorideKHS101 is a small-molecule inhibitor of TACC3, which is a key component of centrosome-microtubule dynamic networks. |
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| S1233 |
2-Methoxyestradiol (2-MeOE2)2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) 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. |
-S123306W0220150907.gif)
-S123306W0220150907.gif)
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.
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| 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. |
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| S3374 |
Verubulin hydrochlorideVerubulin hydrochloride(MPC 6827 hydrochloride) is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals. |
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| S0360 |
EGFR InhibitorEGFR 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. |
| 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 (NSC 125973)Paclitaxel (NSC 125973, PTX, Taxol, Onxal, Abraxane) is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells. |
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. |
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| S1148 |
Docetaxel (RP56976)Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
|
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| S1241 |
Vincristine (NSC-67574) sulfateVincristine sulfate (NSC-67574, Leurocristine, Oncovin, 22-Oxovincaleukoblastine) 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. |
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 EC0.01 of 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. |
|
| E2402新 |
T-1101 tosylateT-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. |
||
| S8912新 |
Eribulin Mesylate (E7389)Eribulin Mesylate (E7389, B-1939, ER-086526), an analogue of the marine natural product halichondrin B, is a nontaxane completely synthetic microtubule inhibitor. |
||
| S6954新 |
CK-869CK-869 (CK 0157869) is a small molecule inhibitor of actin-related protein 2/3 (Arp2/3) complex with an IC50 of 7 μM. CK-869 can directly suppresses microtubule assembly both in vitro and in vivo. |
||
| 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. |
Cell viability in H292 monolayer cells after 3-day treatment and spheroid volume in H292 3D cultureafter 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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| S2775 |
Nocodazole (R17934)Nocodazole (R17934, Oncodazole, NSC238159) 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. |
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. |
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| S3022 |
Cabazitaxel (XRP6258)Cabazitaxel (RPR-116258A, XRP6258, TXD 258, Taxoid XRP6258) 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. |
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. |
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| 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. |
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. |
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| S1297 |
Epothilone AEpothilone A is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 2 μM. |
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| S7204 |
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) DisodiumFosbretabulin (Combretastatin A4 Phosphate, CA4P, CA 4DP) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd 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. |
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 |
Albendazole (SKF-62979)Albendazole (SKF-62979) is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations. |
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 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over 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 (Ricobendazole) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations. |
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| S2440 |
Vindesine sulfateVindesine 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. |
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| S5256 |
Benproperine phosphateBenproperine phosphate (Blascorid, Pirexyl), a cough suppressant, is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate suppresses cancer cell migration and tumor metastasis. |
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| S7721 |
Monomethyl auristatin E (MMAE)Monomethyl auristatin E (MMAE, SGD-1010) is a synthetic antineoplastic agent, which is linked to a monoclonal antibody (MAB). It is also a microtubule-disrupting agent . |
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| S4114 |
TriclabendazoleTriclabendazole (CGA-89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis. |
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| S3970 |
VindolineVindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly. |
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| S8789 |
SSE15206SSE15206 is a tubulin polymerization inhibitor that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents. |
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| S7787 |
Docetaxel TrihydrateDocetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
(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. |
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| 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. |
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| S7783 |
Combretastatin A4Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3. |
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| S0328 |
MMAFMMAF (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. |
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| S2284 |
Colchicine (NSC 757)Colchicine (NSC 757, Colchineos, Colchisol, Colcin) is a microtubule polymerization inhibitor with an IC50 of 3 nM. |
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| S2447 |
Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222)Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222, Antibiotic C 15003P3) is a potent inhibitor of tubulin polymerization with IC50 of 3.4 μM. |
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| S4071 |
GriseofulvinGriseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function. |
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| S7762 |
TRx0237 (LMTX) mesylateTRx 0237 mesylate (LMTX, Hydromethylthionine) is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia. |
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| S7497 |
CK-636CK-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. |
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| 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. |
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| S4269 |
Vinorelbine ditartrate (KW-2307)Vinorelbine Tartrate (KW-2307, Nor-5'-anhydrovinblastine ditartrate) 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. |
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.
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| S6661 |
VcMMAEVcMMAE (mc-vc-PAB-MMAE), a MMAE derivative with valine-citrulline (Vc) linker,is an Drug-linker Conjugate for 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. |
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| S7495 |
TAI-1TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction. |
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| S7930 |
Ixabepilone (BMS-247550)Ixabepilone (BMS-247550, Azaepothilone B, BMS 247550-1, Ixempra, Aza-epothilone B) 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. |
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| S4505 |
Vinblastine (NSC-49842) sulfateVinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) 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. |
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| S7493 |
INH1INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction. |
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| S6773 |
MertansineMertansine (DM1, Maytansinoid DM1), an antibody-conjugatable maytansinoid, is a selective microtubule inhibitor that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC). Solutions are best fresh-prepared. |
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| S7494 |
INH6INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment. |
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| S3206 |
5a-Pregnane-3,20-dione5a-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. |
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| S0444 |
IndibulinIndibulin (ZIO 301, D 24851, Zybulin) is an orally applied inhibitor of tubulin assembly with potent anticancer activity. Indibulin induces mitotic arrest and apoptosis. |
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| S4535 |
Methylene BlueMethylene 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. |
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| S2441 |
Estramustine phosphate sodiumEstramustine phosphate sodium (EMP, Emcyt, Estracyt) 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. |
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| S2444 |
ParbendazoleParbendazole (SKF 29044) is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules. |
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| S9555 |
VincristineVincristine (Leurocristine, NSC-67574, 22-Oxovincaleukoblastine) is a natural alkaloid isolated from the plant Vinca rosea Linn. with anti-tumor activity. Vincristine inhibits microtubule formation in mitotic spindle and binds to microtubule with Ki of 85 nM. |
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| S3220 |
TrigonellineTrigonelline (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. |
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| S5919 |
KHS101 hydrochlorideKHS101 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, 2-ME2) 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. |
2022, 79(6):314 2022, 1868(5):166356 2022, 23(8)4171 |
-S123306W0220150907.gif)
-S123306W0220150907.gif)
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.
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| 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. |
2019, 294(20):8161-8170 2019, 96(6):711-719 2013, 5(3):195-212 |
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| S3374 |
Verubulin hydrochlorideVerubulin hydrochloride(MPC 6827 hydrochloride) is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals. |
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| S0360 |
EGFR InhibitorEGFR 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. |
