Microtubule Associated

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S1150 Paclitaxel パクリタキセル (Paclitaxel (NSC 125973, PTX)) は微小管を安定化することで脱重合を阻害します。ヒト血管内皮細胞における IC50 は 0.1 pM です。
Adv Sci (Weinh), 2024, 11(5):e2305035
Cell Death Differ, 2024, 10.1038/s41418-024-01267-9
Clin Transl Med, 2024, 14(2):e1567
S1148 Docetaxel Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
Drug Resist Updat, 2024, 73:101063
Sci Rep, 2024, 14(1):729
Life Sci Alliance, 2024, 7(4)e202302257
S1241 Vincristine sulfate Vincristine sulfate 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.
iScience, 2024, 27(1):108667
Cell Rep Med, 2023, 4(12):101339
Acta Neuropathol Commun, 2023, 11(1):6
S2775 Nocodazole Nocodazole 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.
Life Sci Alliance, 2024, 7(4)e202302257
Nat Metab, 2023, 5(2):277-293
Adv Sci (Weinh), 2023, 10(7):e2205566
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.
Cell Death Dis, 2023, 14(4):234
JCI Insight, 2023, 8(23)e164968
Phytomedicine, 2023, 115:154809
S7787 Docetaxel Trihydrate Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
PLoS Biol, 2023, 21(4):e3002038
Mol Cancer, 2022, 21(1):150
Theranostics, 2022, 12(11):4965-4979
S4505 Vinblastine sulfate Vinblastine sulfate 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.
J Immunother Cancer, 2023, 11(8)e007253
J Immunother Cancer, 2023, 10.1136/jitc-2023-007253
Cell Rep, 2023, 42(4):112324
S4269 Vinorelbine ditartrate Vinorelbine 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.
Cell Rep, 2023, 42(10):113176
J Pathol, 2023, 261(3):256-268
Cell Oncol (Dordr), 2023, 10.1007/s13402-023-00786-w
S3022 Cabazitaxel Cabazitaxel 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.
Sci Adv, 2024, 10(5):eadg7887
Cancer Drug Resist, 2024, 7:3
Biochem Pharmacol, 2023, 214:115681
S2284 Colchicine Colchicine is a microtubule polymerization inhibitor with an IC50 of 3 nM.
Biomedicines, 2024, 12(2)406
Cell Death Discov, 2023, 9(1):245
Nat Commun, 2022, 13(1):4285
S1364 Patupilone (Epothilone B) Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.
Brain Commun, 2023, 5(1):fcad005
Brain, 2022, awac079
J Cell Biol, 2021, 220(12)e202010155
S7930 Ixabepilone Ixabepilone 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.
J Pers Med, 2022, 12(2)258
Pharmacol Rep, 2022, 10.1007/s43440-022-00396-7
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7204 Fosbretabulin (Combretastatin A4 Phosphate) Disodium Fosbretabulin (Combretastatin A4 Phosphate) 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.
Front Oncol, 2023, 13:1249524
Front Oncol, 2023, 13:1249524
Cell, 2020, 182(3):685-712.e19
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.
Cell, 2021, 184(2):334-351.e20
Adv Virol, 2020, 2020:8844061
J Exp Clin Cancer Res, 2019, 38(1):44
S1640 Albendazole Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
Sci Rep, 2022, 12(1):5706
Mol Cell, 2021, 81(19):4041-4058.e15
Cancer Lett, 2021, 520:307-320
S7336 CW069 CW069 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over KSP.
Nat Commun, 2023, 14(1):6505
Life Sci Alliance, 2022, 5(11)e202201470
Mol Biol Cell, 2022, mbcE22030098
S7721 MMAE (Monomethyl auristatin E) MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent.
Leuk Lymphoma, 2023, 1-11.
Br J Haematol, 2022, 10.1111/bjh.18341
Cancer Cell, 2021, S1535-6108(21)00659-0
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
S1176 Plinabulin Plinabulin is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. Phase 1/2.
J Med Chem, 2022, 65(13):9159-9173
ACS Omega, 2022, 7(25):21465-21472
J Biol Chem, 2019, 294(20):8161-8170
S7783 Combretastatin A4 Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3.
Mol Cell, 2023, 83(13):2290-2302.e13
Cell Rep, 2023, 42(10):113176
Mol Cancer Ther, 2020, molcanther.0525.2020
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.
Elife, 2021, 10e65910
Theranostics, 2019, 9(25):7628-7647
Front Cell Infect Microbiol, 2017, 7:400
S1297 Epothilone A Epothilone A is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 2 μM.
Environ Mol Mutagen, 2022, 63(3):151-161
Cancers (Basel), 2020, 12(12)E3816
Sci Rep, 2020, 10(1):13124
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.e5
Curr Biol, 2019, 29(18):3072-3080
S0360 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.
Cell Rep, 2022, 40-8:111223
Cancers (Basel), 2022, 14(19)4910
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.
Cell Res, 2023, 10.1038/s41422-023-00846-8
bioRxiv, 2020, 2020/9/20.4.7.30734
S2440 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
S5256 Benproperine phosphate Benproperine 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 actin polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate suppresses cancer cell migration and tumor metastasis.
Mol Oncol, 2020, 10.1002/1878-0261.12854
S3970 Vindoline Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly.
Nat Commun, 2020, 11(1):941
S9695 iHAP1 iHAP1 is a well-established microtubule poison, blocks microtubule polymerization fully at 5 µM which is independent of deregulated transcription, causes marked sensitization when deleting Rod1 gene in HeLa cells.
J Cell Biol, 2022, 221-11e202202100
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
S0328 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.
Cancer Cell, 2021, S1535-6108(21)00659-0
E1068 Nab-Paclitaxel Nab-Paclitaxel, a novel solvent-free taxane with the binding ratio of Paclitaxel to human serum albumin of 1:9, is an anti-microtubule drug that promotes microtubule aggregation in tubulin dimer and inhibits microtubule depolymerization to stabilize the microtubule system.
J Transl Med, 2023, 21(1):730
S7762 TRx0237 (LMTX) mesylate TRx 0237 mesylate (LMTX, Hydromethylthionine) is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.
Nat Commun, 2023, 14(1):3939
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
S0444 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
S3220 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.
Biomed Pharmacother, 2021, 143:112204
S1836 Albendazole Oxide Albendazole Oxide (Ricobendazole,Albendazole sulfoxide) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.
S0510 Myoseverin Myoseverin is a microtubule-binding trisubstituted purine, reversibly altering cellular function, directly binds tubulin and disrupts the structure of the microtubule cytoskeleton resulting in myotube fission at 20 μM.
S9969New RMC-4630 RMC-4630 (SSE15206) is an inhibitor of microtubule polymerization with a GI50 of 197 nM in HCT116 cells. It can overcome multidrug resistance and cause aberrant mitosis, resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
S4114 Triclabendazole Triclabendazole (CGA-89317,tcbz) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.
S3374 Verubulin hydrochloride Verubulin hydrochloride(MPC 6827 hydrochloride) is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals.
S6954 CK-869 CK-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.
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.
D4003New Trastuzumab Emtansine(T-DM1) Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.This product is supplied as 10mg/ml PBS solution.
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.
S4071 Griseofulvin Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.
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.
S6661 VcMMAE VcMMAE (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.
S6773 Mertansine Mertansine (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 unstable and should be fresh-prepared.
S7494 INH6 INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
S3206 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.
E2402 T-1101 tosylate T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity.
S8912 Eribulin Mesylate Eribulin Mesylate, an analogue of the marine natural product halichondrin B, is a nontaxane completely synthetic microtubule inhibitor.
S2441 Estramustine phosphate sodium Estramustine 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.
S2444 Parbendazole Parbendazole (SKF 29044) is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules.
S9555 Vincristine Vincristine (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.
Sci Bull (Beijing), 2023, 10.1016/j.scib.2023.11.027
EMBO Mol Med, 2023, 15(12):e18199
Cell Death Dis, 2023, 14(1):64
E2851 Trastuzumab-Emtansine(T-DM1) Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.This product is supplied as 10mg/ml PBS solution.
S5919 KHS101 hydrochloride KHS101 is a small-molecule inhibitor of TACC3, which is a key component of centrosome-microtubule dynamic networks.
S1150 Paclitaxel パクリタキセル (Paclitaxel (NSC 125973, PTX)) は微小管を安定化することで脱重合を阻害します。ヒト血管内皮細胞における IC50 は 0.1 pM です。
Adv Sci (Weinh), 2024, 11(5):e2305035
Cell Death Differ, 2024, 10.1038/s41418-024-01267-9
Clin Transl Med, 2024, 14(2):e1567
S1148 Docetaxel Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
Drug Resist Updat, 2024, 73:101063
Sci Rep, 2024, 14(1):729
Life Sci Alliance, 2024, 7(4)e202302257
S1241 Vincristine sulfate Vincristine sulfate 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.
iScience, 2024, 27(1):108667
Cell Rep Med, 2023, 4(12):101339
Acta Neuropathol Commun, 2023, 11(1):6
S2775 Nocodazole Nocodazole 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.
Life Sci Alliance, 2024, 7(4)e202302257
Nat Metab, 2023, 5(2):277-293
Adv Sci (Weinh), 2023, 10(7):e2205566
S7787 Docetaxel Trihydrate Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
PLoS Biol, 2023, 21(4):e3002038
Mol Cancer, 2022, 21(1):150
Theranostics, 2022, 12(11):4965-4979
S4505 Vinblastine sulfate Vinblastine sulfate 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.
J Immunother Cancer, 2023, 11(8)e007253
J Immunother Cancer, 2023, 10.1136/jitc-2023-007253
Cell Rep, 2023, 42(4):112324
S4269 Vinorelbine ditartrate Vinorelbine 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.
Cell Rep, 2023, 42(10):113176
J Pathol, 2023, 261(3):256-268
Cell Oncol (Dordr), 2023, 10.1007/s13402-023-00786-w
S3022 Cabazitaxel Cabazitaxel 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.
Sci Adv, 2024, 10(5):eadg7887
Cancer Drug Resist, 2024, 7:3
Biochem Pharmacol, 2023, 214:115681
S2284 Colchicine Colchicine is a microtubule polymerization inhibitor with an IC50 of 3 nM.
Biomedicines, 2024, 12(2)406
Cell Death Discov, 2023, 9(1):245
Nat Commun, 2022, 13(1):4285
S1364 Patupilone (Epothilone B) Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.
Brain Commun, 2023, 5(1):fcad005
Brain, 2022, awac079
J Cell Biol, 2021, 220(12)e202010155
S7930 Ixabepilone Ixabepilone 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.
J Pers Med, 2022, 12(2)258
Pharmacol Rep, 2022, 10.1007/s43440-022-00396-7
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7204 Fosbretabulin (Combretastatin A4 Phosphate) Disodium Fosbretabulin (Combretastatin A4 Phosphate) 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.
Front Oncol, 2023, 13:1249524
Front Oncol, 2023, 13:1249524
Cell, 2020, 182(3):685-712.e19
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.
Cell, 2021, 184(2):334-351.e20
Adv Virol, 2020, 2020:8844061
J Exp Clin Cancer Res, 2019, 38(1):44
S1640 Albendazole Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
Sci Rep, 2022, 12(1):5706
Mol Cell, 2021, 81(19):4041-4058.e15
Cancer Lett, 2021, 520:307-320
S7336 CW069 CW069 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over KSP.
Nat Commun, 2023, 14(1):6505
Life Sci Alliance, 2022, 5(11)e202201470
Mol Biol Cell, 2022, mbcE22030098
S7721 MMAE (Monomethyl auristatin E) MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent.
Leuk Lymphoma, 2023, 1-11.
Br J Haematol, 2022, 10.1111/bjh.18341
Cancer Cell, 2021, S1535-6108(21)00659-0
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
S7783 Combretastatin A4 Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3.
Mol Cell, 2023, 83(13):2290-2302.e13
Cell Rep, 2023, 42(10):113176
Mol Cancer Ther, 2020, molcanther.0525.2020
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.
Elife, 2021, 10e65910
Theranostics, 2019, 9(25):7628-7647
Front Cell Infect Microbiol, 2017, 7:400
S1297 Epothilone A Epothilone A is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 2 μM.
Environ Mol Mutagen, 2022, 63(3):151-161
Cancers (Basel), 2020, 12(12)E3816
Sci Rep, 2020, 10(1):13124
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.e5
Curr Biol, 2019, 29(18):3072-3080
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.
Cell Res, 2023, 10.1038/s41422-023-00846-8
bioRxiv, 2020, 2020/9/20.4.7.30734
S2440 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
S5256 Benproperine phosphate Benproperine 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 actin polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate suppresses cancer cell migration and tumor metastasis.
Mol Oncol, 2020, 10.1002/1878-0261.12854
S3970 Vindoline Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly.
Nat Commun, 2020, 11(1):941
S9695 iHAP1 iHAP1 is a well-established microtubule poison, blocks microtubule polymerization fully at 5 µM which is independent of deregulated transcription, causes marked sensitization when deleting Rod1 gene in HeLa cells.
J Cell Biol, 2022, 221-11e202202100
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
S0328 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.
Cancer Cell, 2021, S1535-6108(21)00659-0
E1068 Nab-Paclitaxel Nab-Paclitaxel, a novel solvent-free taxane with the binding ratio of Paclitaxel to human serum albumin of 1:9, is an anti-microtubule drug that promotes microtubule aggregation in tubulin dimer and inhibits microtubule depolymerization to stabilize the microtubule system.
J Transl Med, 2023, 21(1):730
S7762 TRx0237 (LMTX) mesylate TRx 0237 mesylate (LMTX, Hydromethylthionine) is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.
Nat Commun, 2023, 14(1):3939
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
S0444 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
S3220 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.
Biomed Pharmacother, 2021, 143:112204
S1836 Albendazole Oxide Albendazole Oxide (Ricobendazole,Albendazole sulfoxide) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.
S0510 Myoseverin Myoseverin is a microtubule-binding trisubstituted purine, reversibly altering cellular function, directly binds tubulin and disrupts the structure of the microtubule cytoskeleton resulting in myotube fission at 20 μM.
S9969New RMC-4630 RMC-4630 (SSE15206) is an inhibitor of microtubule polymerization with a GI50 of 197 nM in HCT116 cells. It can overcome multidrug resistance and cause aberrant mitosis, resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
S4114 Triclabendazole Triclabendazole (CGA-89317,tcbz) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.
S6954 CK-869 CK-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.
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.
D4003New Trastuzumab Emtansine(T-DM1) Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.This product is supplied as 10mg/ml PBS solution.
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.
S4071 Griseofulvin Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.
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.
S6661 VcMMAE VcMMAE (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.
S6773 Mertansine Mertansine (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 unstable and should be fresh-prepared.
S7494 INH6 INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
S3206 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.
E2402 T-1101 tosylate T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity.
S8912 Eribulin Mesylate Eribulin Mesylate, an analogue of the marine natural product halichondrin B, is a nontaxane completely synthetic microtubule inhibitor.
S2441 Estramustine phosphate sodium Estramustine 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.
S2444 Parbendazole Parbendazole (SKF 29044) is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules.
S9555 Vincristine Vincristine (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.
Sci Bull (Beijing), 2023, 10.1016/j.scib.2023.11.027
EMBO Mol Med, 2023, 15(12):e18199
Cell Death Dis, 2023, 14(1):64
E2851 Trastuzumab-Emtansine(T-DM1) Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.This product is supplied as 10mg/ml PBS solution.
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, 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.
Cell Death Dis, 2023, 14(4):234
JCI Insight, 2023, 8(23)e164968
Phytomedicine, 2023, 115:154809
S1176 Plinabulin Plinabulin is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. Phase 1/2.
J Med Chem, 2022, 65(13):9159-9173
ACS Omega, 2022, 7(25):21465-21472
J Biol Chem, 2019, 294(20):8161-8170
S0360 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.
Cell Rep, 2022, 40-8:111223
Cancers (Basel), 2022, 14(19)4910
S3374 Verubulin hydrochloride Verubulin hydrochloride(MPC 6827 hydrochloride) is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals.
S9969New RMC-4630 RMC-4630 (SSE15206) is an inhibitor of microtubule polymerization with a GI50 of 197 nM in HCT116 cells. It can overcome multidrug resistance and cause aberrant mitosis, resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
D4003New Trastuzumab Emtansine(T-DM1) Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.This product is supplied as 10mg/ml PBS solution.

Microtubule Associated阻害剤の選択性比較

Microtubule Associatedシグナル伝達経路

Microtubule Associatedシグナル伝達経路
Tags: microtubule inhibition | microtubule drugs | microtubule cancer | microtubule assay | microtubule phosphorylation | tubulin pathway | microtubule poison | microtubule inhibitors cancer | microtubule inhibitor drugs | microtubule inhibitor review