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。 |
-
Bioact Mater, 2025, 43:67-81
-
Nat Commun, 2024, 15(1):2503
-
Nat Commun, 2024, 15(1):2089
|
|
S1148 |
Docetaxel
|
Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
-
Nature, 2024, 10.1038/s41586-024-08031-6
-
Cell Discov, 2024, 10(1):39
-
Drug Resist Updat, 2024, 73:101063
|
|
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. |
-
Nat Commun, 2024, 15(1):4513
-
Nat Commun, 2024, 15(1):4739
-
iScience, 2024, 27(1):108667
|
|
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. |
-
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
-
Nat Commun, 2024, 15(1):9771
-
Nucleic Acids Res, 2024, gkae605
|
|
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. |
-
Theranostics, 2024, 14(13):5123-5140
-
Int J Biol Sci, 2024, 20(6):2323-2338
-
J Transl Med, 2024, 22(1):649
|
|
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. |
-
Int J Mol Sci, 2024, 25(21)11346
-
PLoS One, 2024, 19(11):e0307153
-
Nat Commun, 2023, 14(1):7576
|
|
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. |
-
BMC Pharmacol Toxicol, 2024, 25(1):25
-
BMC Pharmacol Toxicol, 2024, 25(1):25
-
Cell Rep, 2023, 42(10):113176
|
|
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. |
-
J Photochem Photobiol B, 2024, 253:112877
-
Cancer Biol Ther, 2024, 25(1):2329368
-
Sci Adv, 2024, 10(5):eadg7887
|
|
S2284 |
Colchicine
|
Colchicine is a microtubule polymerization inhibitor with an IC50 of 3 nM. |
-
Biomedicines, 2024, 12(2)406
-
Front Physiol, 2024, 15:1425620
-
ACS Chem Biol, 2024, 19(8):1733-1742
|
|
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
-
Nat Commun, 2023, 14(1):6505
-
Life Sci Alliance, 2022, 5(11)e202201470
|
|
S7721 |
MMAE (Monomethyl auristatin E)
|
MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent.
|
-
Front Immunol, 2024, 15:1393485
-
Leuk Lymphoma, 2023, 1-11.
-
Br J Haematol, 2022, 10.1111/bjh.18341
|
|
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
-
Mol Cell, 2023, 83(13):2290-2302.e13
-
Cell Rep, 2023, 42(10):113176
|
|
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, 2024, 10.1002/em.22604
-
Environ Mol Mutagen, 2022, 63(3):151-161
-
Cancers (Basel), 2020, 12(12)E3816
|
|
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
|
|
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. Solutions are unstable and should be fresh-prepared. |
-
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. |
|
|
S2440 |
Vindesine sulfate
|
Vindesine sulfate, 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
|
|
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. |
|
|
S9969 |
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. |
-
Arch Biochem Biophys, 2024, 754:109958
|
|
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. |
|
|
E1426New |
EAPB02303
|
EAPB02303 is a second-generation imiqualine that acts as a microtubule -disruptingagent and demonstrates anti-tumor effects and reduces tumor size in human melanoma xenografts. |
|
|
D4003 |
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. |
|
|
E4897New |
Estramustine
|
Estramustine(NSC-89201, LEO275) is used to treat hormone-resistant prostate cancer and stabilize microtubule dynamics. It acts as an anti-mitotic and anti-microtubule agent and disrupts microtubule disassembly. It inhibits the binding of MAPs 1 and 2 to taxol-stabilized microtubules, hinders microtubule assembly, and promotes the disassembly of MAP-2-associated microtubules. |
|
|
S4071 |
Griseofulvin
|
Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function. |
-
Leukemia, 2024, 38(5):969-980
|
|
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. |
|
|
A2692 |
Gosuranemab (Anti-Tau)
|
Gosuranemab (Anti-Tau) is a humanized monoclonal antibody against the extracellular N-terminal of tau in the interstitial fluid (ISF) and CSF released by neurons. It has the potential for research of alzheimer’s disease (AD). MW : 150 kD. |
|
|
A2693 |
Semorinemab (Anti-Tau)
|
Semorinemab (Anti-Tau) is a humanized IgG4 monoclonal antibody that targets the N-terminal domain of tau (amino acid residues 6-23). Semorinemab has the potential to be used in research on Alzheimer's disease. MW : 150 kD. |
|
|
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 |
DM1 (Mertansine)
|
DM1 (Mertansine), 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. |
-
Front Pharmacol, 2024, 15:1459820
-
Biomolecules, 2024, 14(7)741
-
Am J Cancer Res, 2024, 14(7):3388-3403
|
|
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. |
|
|
A2341 |
Zagotenemab (Anti-Tau)
|
Zagotenemab (Anti-Tau) is a humanised anti-tau antibody that selectively binds and neutralises tau deposits in the brain. It has the potential to be used in Alzheimer's disease research. MW : 145.5 KD |
|
|
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。 |
- Bioact Mater, 2025, 43:67-81
- Nat Commun, 2024, 15(1):2503
- Nat Commun, 2024, 15(1):2089
|
|
S1148 |
Docetaxel
|
Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
- Nature, 2024, 10.1038/s41586-024-08031-6
- Cell Discov, 2024, 10(1):39
- Drug Resist Updat, 2024, 73:101063
|
|
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. |
- Nat Commun, 2024, 15(1):4513
- Nat Commun, 2024, 15(1):4739
- iScience, 2024, 27(1):108667
|
|
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. |
- Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
- Nat Commun, 2024, 15(1):9771
- Nucleic Acids Res, 2024, gkae605
|
|
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. |
- Int J Mol Sci, 2024, 25(21)11346
- PLoS One, 2024, 19(11):e0307153
- Nat Commun, 2023, 14(1):7576
|
|
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. |
- BMC Pharmacol Toxicol, 2024, 25(1):25
- BMC Pharmacol Toxicol, 2024, 25(1):25
- Cell Rep, 2023, 42(10):113176
|
|
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. |
- J Photochem Photobiol B, 2024, 253:112877
- Cancer Biol Ther, 2024, 25(1):2329368
- Sci Adv, 2024, 10(5):eadg7887
|
|
S2284 |
Colchicine
|
Colchicine is a microtubule polymerization inhibitor with an IC50 of 3 nM. |
- Biomedicines, 2024, 12(2)406
- Front Physiol, 2024, 15:1425620
- ACS Chem Biol, 2024, 19(8):1733-1742
|
|
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
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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
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S2195 |
Lexibulin (CYT997)
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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
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S1640 |
Albendazole
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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
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S7336 |
CW069
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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
- Nat Commun, 2023, 14(1):6505
- Life Sci Alliance, 2022, 5(11)e202201470
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S7721 |
MMAE (Monomethyl auristatin E)
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MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent.
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- Front Immunol, 2024, 15:1393485
- Leuk Lymphoma, 2023, 1-11.
- Br J Haematol, 2022, 10.1111/bjh.18341
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S1165 |
ABT-751 (E7010)
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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
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S7783 |
Combretastatin A4
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Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3.
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- Mol Cell, 2023, 83(13):2290-2302.e13
- Mol Cell, 2023, 83(13):2290-2302.e13
- Cell Rep, 2023, 42(10):113176
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S7497 |
CK-636
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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
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S1297 |
Epothilone A
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Epothilone A is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 2 μM. |
- Environ Mol Mutagen, 2024, 10.1002/em.22604
- Environ Mol Mutagen, 2022, 63(3):151-161
- Cancers (Basel), 2020, 12(12)E3816
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S7495 |
TAI-1
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TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.
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- 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
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S4535 |
Methylene Blue
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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
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S5256 |
Benproperine phosphate
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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
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S3970 |
Vindoline
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Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly. |
- Nat Commun, 2020, 11(1):941
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S9695 |
iHAP1
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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
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S2254 |
4-Demethylepipodophyllotoxin(NSC-122819,VM-26)
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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
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S0328 |
MMAF
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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
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E1068 |
Nab-Paclitaxel
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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. Solutions are unstable and should be fresh-prepared. |
- J Transl Med, 2023, 21(1):730
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S7762 |
TRx0237 (LMTX) mesylate
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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
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S7493 |
INH1
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INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.
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- J Clin Invest, 2018, 128(7):2877-2893
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S0444 |
Indibulin
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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
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S3220 |
Trigonelline
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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
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S1836 |
Albendazole Oxide
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Albendazole Oxide (Ricobendazole,Albendazole sulfoxide) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations. |
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S2440 |
Vindesine sulfate
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Vindesine sulfate, 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
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S0510 |
Myoseverin
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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. |
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S9969 |
RMC-4630
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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. |
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S4114 |
Triclabendazole
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Triclabendazole (CGA-89317,tcbz) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis. |
- Arch Biochem Biophys, 2024, 754:109958
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S6954 |
CK-869
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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. |
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S8789 |
SSE15206
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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. |
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E1426New |
EAPB02303
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EAPB02303 is a second-generation imiqualine that acts as a microtubule -disruptingagent and demonstrates anti-tumor effects and reduces tumor size in human melanoma xenografts. |
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D4003 |
Trastuzumab Emtansine(T-DM1)
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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. |
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S2447 |
Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222)
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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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E4897New |
Estramustine
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Estramustine(NSC-89201, LEO275) is used to treat hormone-resistant prostate cancer and stabilize microtubule dynamics. It acts as an anti-mitotic and anti-microtubule agent and disrupts microtubule disassembly. It inhibits the binding of MAPs 1 and 2 to taxol-stabilized microtubules, hinders microtubule assembly, and promotes the disassembly of MAP-2-associated microtubules. |
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S4071 |
Griseofulvin
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Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function. |
- Leukemia, 2024, 38(5):969-980
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S3725 |
ELR-510444
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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. |
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S6661 |
VcMMAE
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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. |
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S6773 |
DM1 (Mertansine)
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DM1 (Mertansine), 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. |
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S7494 |
INH6
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INH6 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-dione
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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. |
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E2402 |
T-1101 tosylate
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T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. |
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S8912 |
Eribulin Mesylate
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Eribulin Mesylate, an analogue of the marine natural product halichondrin B, is a nontaxane completely synthetic microtubule inhibitor. |
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S2441 |
Estramustine phosphate sodium
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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. |
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S2444 |
Parbendazole
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Parbendazole (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 |
Vincristine
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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. |
- Front Pharmacol, 2024, 15:1459820
- Biomolecules, 2024, 14(7)741
- Am J Cancer Res, 2024, 14(7):3388-3403
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E2851 |
Trastuzumab-Emtansine(T-DM1)
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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. |
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S5919 |
KHS101 hydrochloride
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KHS101 is a small-molecule inhibitor of TACC3, which is a key component of centrosome-microtubule dynamic networks. |
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