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
|
|
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
|
|
S1148 |
Docetaxel (RP56976)
|
Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
-
Cancers (Basel), 2022, 14(4)949
-
Cancers (Basel), 2022, 14(4)928
-
Sci Rep, 2022, 12(1):1442
|
|
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. |
-
Cell Res, 2022, 10.1038/s41422-022-00651-9
-
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
-
Mol Cell, 2022, 82(1):75-89.e9
|
|
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
|
|
S1241 |
Vincristine (NSC-67574) sulfate
|
Vincristine 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. |
-
Nat Cell Biol, 2022, 10.1038/s41556-021-00814-7
-
Mol Cell, 2022, 82(1):75-89.e9
-
Haematologica, 2022, 10.3324/haematol.2021.279957
|
|
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
|
|
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, 2022, awac079
-
J Cell Biol, 2021, 220(12)e202010155
-
Biochem Pharmacol, 2021, 193:114789
|
|
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. |
-
Sci Rep, 2022, 12(1):5706
-
Mol Cell, 2021, 81(19):4041-4058.e15
-
Cancer Lett, 2021, 520:307-320
|
|
S1836 |
Albendazole Oxide
|
Albendazole Oxide (Ricobendazole) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations. |
|
|
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
|
|
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
|
|
S2284 |
Colchicine (NSC 757)
|
Colchicine (NSC 757, Colchineos, Colchisol, Colcin) is a microtubule polymerization inhibitor with an IC50 of 3 nM. |
-
Transl Stroke Res, 2022, 10.1007/s12975-022-01022-7
-
Eur J Pharmacol, 2022, 919:174802
-
Biochem Biophys Res Commun, 2022, 594:161-167
|
|
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
|
|
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.
|
|
|
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. |
|
|
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. |
-
Signal Transduct Target Ther, 2022, 7(1):97
-
Front Cell Dev Biol, 2022, 10:817831
-
J Biol Chem, 2022, S0021-9258(22)00072-2
|
|
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. |
-
Mol Cancer Ther, 2021, molcanther.0983.2020
-
Prostate, 2021, 10.1002/pros.24138
-
Prostate, 2021, 10.1002/pros.24200
|
|
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. |
|
|
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
|
|
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. |
|
|
S3970 |
Vindoline
|
Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly. |
-
Nat Commun, 2020, 11(1):941
|
|
S4071 |
Griseofulvin
|
Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function. |
|
|
S4114 |
Triclabendazole
|
Triclabendazole (CGA-89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis. |
|
|
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. |
-
Transl Lung Cancer Res, 2022, 11(4):543-559
-
Cancer Res, 2021, canres.0955.2021
-
Br J Cancer, 2021, 10.1038/s41416-021-01420-y
|
|
S4505 |
Vinblastine (NSC-49842) sulfate
|
Vinblastine 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. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
-
Cancer Res, 2021, canres.0955.2021
|
|
S4535 |
Methylene Blue
|
Methylene Blue (Basic Blue 9, Tetramethylthionine chloride, methylthioninium chloride, CI-52015) is used as a dye in chromoendoscopy. It Inhibits tau filament formation with IC50 of 1.9μM. Also it inhibits soluble guanylyl cyclase. |
-
bioRxiv, 2020, 2020/9/20.4.7.30734
|
|
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 action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate suppresses cancer cell migration and tumor metastasis. |
-
Mol Oncol, 2020, 10.1002/1878-0261.12854
|
|
S5919 |
KHS101 hydrochloride
|
KHS101 is a small-molecule inhibitor of TACC3, which is a key component of centrosome-microtubule dynamic networks. |
|
|
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. |
|
|
S6773New |
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 best fresh-prepared. |
|
|
S6954New |
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. |
|
|
S7204 |
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium
|
Fosbretabulin (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. |
-
Cell, 2020, 182(3):685-712.e19
-
Cell, 2020, 182(3):685-712.e19
-
J Drug Target, 2020, 10.1080/1061186X.2020.1818759
|
|
S7336 |
CW069
|
CW069 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over KSP. |
-
EMBO Rep, 2020, 9:e49234
-
Mol Syst Biol, 2018, 14(8):e8238
-
Anticancer Res, 2018, 38(6):3393-3400
|
|
S7493 |
INH1
|
INH1 (IBT 13131) is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.
|
-
J Clin Invest, 2018, 128(7):2877-2893
|
|
S7494 |
INH6
|
INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
|
|
|
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
|
|
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
|
|
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 .
|
-
Cancer Cell, 2021, S1535-6108(21)00659-0
-
Oncol Lett, 2021, 21(5):397
-
PaDUA, 2019, N/A
|
|
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. |
|
|
S7783 |
Combretastatin A4
|
Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3.
|
-
Mol Cancer Ther, 2020, molcanther.0525.2020
-
Mol Pharmacol, 2019, 96(6):711-719
-
Drug Des Devel Ther, 2017, 11:1335-1351
|
|
S7787 |
Docetaxel Trihydrate
|
Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
|
-
Sci Rep, 2022, 12(1):1442
-
Anal Cell Pathol (Amst), 2022, 2022:8708202
-
Bioengineered, 2022, 13(4):11310-11320
|
|
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. |
-
Environ Mol Mutagen, 2022, 63(3):151-161
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Genome Med, 2021, 13(1):103
|
|
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. |
|
|
S8912New |
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.
|
|
|
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. |
-
Haematologica, 2022, 10.3324/haematol.2021.279957
-
Dis Model Mech, 2022, dmm.049109
-
J Gastroenterol Hepatol, 2022, 10.1111/jgh.15775
|
|
A5106 |
Lamin B1 Rabbit Recombinant mAb
|
Lamin B1 Rabbit Recombinant mAb detects endogenous levels of total Lamin B1. |
|
|
A5107 |
beta Tubulin III Rabbit Recombinant mAb
|
beta Tubulin III Rabbit Recombinant mAb detects endogenous levels of total beta Tubulin III. |
|
|
A5167 |
Beta Tubulin Rabbit Recombinant mAb (HRP conjugated)
|
Beta Tubulin Rabbit Recombinant mAb (HRP conjugated) detects endogenous level of total beta tubulin. |
|
|
A5204 |
67kDa Laminin Receptor Rabbit Recombinant mAb
|
67kDa Laminin Receptor Rabbit Recombinant mAb detects endogenous level of total 67kDa Laminin Receptor. |
|
|
A5228 |
Filamin A Rabbit Recombinant mAb
|
Filamin A Rabbit Recombinant mAb detects endogenous level of Filamin A. |
|
|
A5230 |
Cytokeratin 19 Rabbit Recombinant mAb
|
Cytokeratin 19 Rabbit Recombinant mAb detects endogenous level of total cytokeration 19. |
|
|
A5234 |
Stathmin 1 Rabbit Recombinant mAb
|
Stathmin 1 Rabbit Recombinant mAb detects endogenous level of total Stathmin 1. |
|
|
A5249 |
Cytokeratin 7 Rabbit Recombinant mAb
|
Cytokeratin 7 Rabbit Recombinant mAb detects endogenous level of total Cytokeratin 7. |
|
|
A5253 |
Desmin Rabbit Recombinant mAb
|
Desmin Rabbit Recombinant mAb detects endogenous level of total desmin. |
|
|
A5266 |
Cytokeratin 10 Rabbit Recombinant mAb
|
Cytokeratin 10 Rabbit Recombinant mAb detects endogenous level of total Cytokeratin 10. |
-
Bioact Mater, 2022, 9:523-540
|
|
A5280 |
Radixin Rabbit Recombinant mAb
|
Radixin Rabbit Recombinant mAb detects endogenous level of total Radixin. |
|
|
A5281 |
Ezrin Rabbit Recombinant mAb
|
Ezrin Rabbit Recombinant mAb detects endogenous level of total Ezrin. |
|
|
A5295 |
NEFM Rabbit Recombinant mAb
|
NEFM Rabbit Recombinant mAb detects endogenous level of total NEFM. |
|
|
A5309 |
Drebrin Rabbit Recombinant mAb
|
Drebrin Rabbit Recombinant mAb detects endogenous level of total Drebrin. |
|
|
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. |
|
|
S1176 |
Plinabulin (NPI-2358)
|
Plinabulin (NPI-2358) is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells. Phase 1/2. |
-
J Biol Chem, 2019, 294(20):8161-8170
-
Mol Pharmacol, 2019, 96(6):711-719
-
Curr Protoc Chem Biol, 2013, 5(3):195-212
|
|
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. |
-
Biochim Biophys Acta Mol Basis Dis, 2022, 1868(5):166356
-
Mol Cancer Res, 2022, 20(1):161-175
-
Cell Transplant, 2022, 31:9636897211073127
|
|
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. |
|
|
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
|
|
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
|
|
S1148 |
Docetaxel (RP56976)
|
Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules. |
- Cancers (Basel), 2022, 14(4)949
- Cancers (Basel), 2022, 14(4)928
- Sci Rep, 2022, 12(1):1442
|
|
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. |
- Cell Res, 2022, 10.1038/s41422-022-00651-9
- Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
- Mol Cell, 2022, 82(1):75-89.e9
|
|
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
|
|
S1241 |
Vincristine (NSC-67574) sulfate
|
Vincristine 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. |
- Nat Cell Biol, 2022, 10.1038/s41556-021-00814-7
- Mol Cell, 2022, 82(1):75-89.e9
- Haematologica, 2022, 10.3324/haematol.2021.279957
|
|
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
|
|
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, 2022, awac079
- J Cell Biol, 2021, 220(12)e202010155
- Biochem Pharmacol, 2021, 193:114789
|
|
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. |
- Sci Rep, 2022, 12(1):5706
- Mol Cell, 2021, 81(19):4041-4058.e15
- Cancer Lett, 2021, 520:307-320
|
|
S1836 |
Albendazole Oxide
|
Albendazole Oxide (Ricobendazole) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations. |
|
|
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
|
|
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
|
|
S2284 |
Colchicine (NSC 757)
|
Colchicine (NSC 757, Colchineos, Colchisol, Colcin) is a microtubule polymerization inhibitor with an IC50 of 3 nM. |
- Transl Stroke Res, 2022, 10.1007/s12975-022-01022-7
- Eur J Pharmacol, 2022, 919:174802
- Biochem Biophys Res Commun, 2022, 594:161-167
|
|
S2440 |
Vindesine sulfate
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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
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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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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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S2775 |
Nocodazole (R17934)
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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. |
- Signal Transduct Target Ther, 2022, 7(1):97
- Front Cell Dev Biol, 2022, 10:817831
- J Biol Chem, 2022, S0021-9258(22)00072-2
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S3022 |
Cabazitaxel (XRP6258)
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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. |
- Mol Cancer Ther, 2021, molcanther.0983.2020
- Prostate, 2021, 10.1002/pros.24138
- Prostate, 2021, 10.1002/pros.24200
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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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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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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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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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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. |
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S4114 |
Triclabendazole
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Triclabendazole (CGA-89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis. |
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S4269 |
Vinorelbine ditartrate (KW-2307)
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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. |
- Transl Lung Cancer Res, 2022, 11(4):543-559
- Cancer Res, 2021, canres.0955.2021
- Br J Cancer, 2021, 10.1038/s41416-021-01420-y
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S4505 |
Vinblastine (NSC-49842) sulfate
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Vinblastine 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. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
- Cancer Res, 2021, canres.0955.2021
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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. |
- 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 action 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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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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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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S6773New |
Mertansine
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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 best fresh-prepared. |
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S6954New |
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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S7204 |
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium
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Fosbretabulin (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. |
- Cell, 2020, 182(3):685-712.e19
- Cell, 2020, 182(3):685-712.e19
- J Drug Target, 2020, 10.1080/1061186X.2020.1818759
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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. |
- EMBO Rep, 2020, 9:e49234
- Mol Syst Biol, 2018, 14(8):e8238
- Anticancer Res, 2018, 38(6):3393-3400
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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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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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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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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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S7721 |
Monomethyl auristatin E (MMAE)
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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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- Cancer Cell, 2021, S1535-6108(21)00659-0
- Oncol Lett, 2021, 21(5):397
- PaDUA, 2019, N/A
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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. |
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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 Cancer Ther, 2020, molcanther.0525.2020
- Mol Pharmacol, 2019, 96(6):711-719
- Drug Des Devel Ther, 2017, 11:1335-1351
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S7787 |
Docetaxel Trihydrate
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Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.
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- Sci Rep, 2022, 12(1):1442
- Anal Cell Pathol (Amst), 2022, 2022:8708202
- Bioengineered, 2022, 13(4):11310-11320
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S7930 |
Ixabepilone (BMS-247550)
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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. |
- Environ Mol Mutagen, 2022, 63(3):151-161
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Genome Med, 2021, 13(1):103
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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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S8912New |
Eribulin Mesylate (E7389)
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Eribulin Mesylate (E7389, B-1939, ER-086526), an analogue of the marine natural product halichondrin B, is a nontaxane completely synthetic microtubule inhibitor.
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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. |
- Haematologica, 2022, 10.3324/haematol.2021.279957
- Dis Model Mech, 2022, dmm.049109
- J Gastroenterol Hepatol, 2022, 10.1111/jgh.15775
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