Microtubule Associated

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Microtubule Associated Products

Catalog No. Information Product Use Citations Product Validations
S1150

Paclitaxel

Paclitaxel (NSC 125973, PTX, Taxol, Onxal) is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.

S1148

Docetaxel

Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

S1241

Vincristine sulfate

Vincristine sulfate (Leurocristine) is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.

S1364

Patupilone (Epothilone B)

Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.

S3220New

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.

S3206New

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.

S2440New

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.

S0444New

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.

S0328New

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.

S0360New

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.

S2441New

Estramustine phosphate sodium

Estramustine phosphate sodium is an antitumour drug with a unique dual mode of action. Estrone and estradiol, products of the metabolism of estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels. Estramustine(the cytotoxic metabolite produced by dephosphorylation of estramustine phosphate sodium) is an antiprostatic tumor drug with antimicrotubule effects.

S2444New

Parbendazole

Parbendazole is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules.

S6661New

VcMMAE

VcMMAE (mc-vc-PAB-MMAE), a MMAE derivative with valine-citrulline (Vc) linker,is an antibody-drug conjugate (ADC) with potent antitumor activity. MMAE is a synthetic antineoplastic agent and can be efficiently released from VcMMAE in vitro and exert cytotoxic activity.

S6765New

MMAD

MMAD (Demethyldolastatin 10, Monomethylauristatin D, Monomethyl Dolastatin 10) is a highly toxic inhibitor of tubulin.

S1165

ABT-751 (E7010)

ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.

S2775

Nocodazole

Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.

S3022

Cabazitaxel

Cabazitaxel (RPR-116258A, XRP6258, TXD 258) is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.

S2195

Lexibulin (CYT997)

Lexibulin (CYT997) is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. Phase 2.

S1297

Epothilone A

Epothilone A is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 2 μM.

S7204

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with 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.

S1640

Albendazole

Albendazole (SKF-62979) is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.

S7336

CW069

CW069 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over KSP.

S1836

Albendazole Oxide

Albendazole Oxide (Ricobendazole) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.

S7721

Monomethyl auristatin E (MMAE)

Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent, which is linked to a monoclonal antibody (MAB). It is also a microtubule-disrupting agent .

S4114

Triclabendazole

Triclabendazole (CGA-89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.

S3970

Vindoline

Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly.

S8789

SSE15206

SSE15206 is a tubulin polymerization inhibitor that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents.

S7787

Docetaxel Trihydrate

Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

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.

S7783

Combretastatin A4

Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3.

S2284

Colchicine

Colchicine (Colchineos, Colchisol, Colcin) is a microtubule polymerization inhibitor with an IC50 of 3 nM.

S4071

Griseofulvin

Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.

S7762

TRx0237 (LMTX) mesylate

TRx 0237 (LMTX™) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.

S7497

CK-636

CK-636 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.

S3725

ELR-510444

ELR-510444 is a novel microtubule disruptor with potential antivascular effects and in vivo antitumor efficacy, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells.

S4269

Vinorelbine Tartrate

Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.

S7495

TAI-1

TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.

S7930

Ixabepilone (BMS-247550)

Ixabepilone (BMS-247550, Azaepothilone B, BMS 247550-1, Ixempra) is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis.

S4505

Vinblastine sulfate

Vinblastine sulfate (NSC49842) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.

S7493

INH1

INH1 is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.

S7494

INH6

INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.

S4535

Methylene Blue

Methylene Blue is used as a dye in chromoendoscopy. It Inhibits tau filament formation with IC50 of 1.9μM. Also it inhibits soluble guanylyl cyclase.

S5919

KHS101 hydrochloride

KHS101 is a small-molecule inhibitor of TACC3, which is a key component of centrosome-microtubule dynamic networks.

S1233

2-Methoxyestradiol (2-MeOE2)

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

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.

Catalog No. Information Product Use Citations Product Validations
S1150

Paclitaxel

Paclitaxel (NSC 125973, PTX, Taxol, Onxal) is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.

S1148

Docetaxel

Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

S1241

Vincristine sulfate

Vincristine sulfate (Leurocristine) is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.

S1364

Patupilone (Epothilone B)

Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 1.8 μM. Phase 2.

S3220New

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.

S3206New

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.

S2440New

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.

S0444New

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.

S0328New

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.

S0360New

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.

S2441New

Estramustine phosphate sodium

Estramustine phosphate sodium is an antitumour drug with a unique dual mode of action. Estrone and estradiol, products of the metabolism of estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels. Estramustine(the cytotoxic metabolite produced by dephosphorylation of estramustine phosphate sodium) is an antiprostatic tumor drug with antimicrotubule effects.

S2444New

Parbendazole

Parbendazole is an extremely potent inhibitor of microtubule assembly with IC50 of 3 µM for the assembly of brain microtubules.

S6661New

VcMMAE

VcMMAE (mc-vc-PAB-MMAE), a MMAE derivative with valine-citrulline (Vc) linker,is an antibody-drug conjugate (ADC) with potent antitumor activity. MMAE is a synthetic antineoplastic agent and can be efficiently released from VcMMAE in vitro and exert cytotoxic activity.

S6765New

MMAD

MMAD (Demethyldolastatin 10, Monomethylauristatin D, Monomethyl Dolastatin 10) is a highly toxic inhibitor of tubulin.

S1165

ABT-751 (E7010)

ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.

S2775

Nocodazole

Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.

S3022

Cabazitaxel

Cabazitaxel (RPR-116258A, XRP6258, TXD 258) is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.

S2195

Lexibulin (CYT997)

Lexibulin (CYT997) is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. Phase 2.

S1297

Epothilone A

Epothilone A is a paclitaxel-like microtubule-stabilizing agent with EC0.01 of 2 μM.

S7204

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with 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.

S1640

Albendazole

Albendazole (SKF-62979) is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.

S7336

CW069

CW069 is an allosteric, and selective inhibitor of microtubule motor protein HSET with IC50 of 75 μM, significant selectivity over KSP.

S1836

Albendazole Oxide

Albendazole Oxide (Ricobendazole) is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.

S7721

Monomethyl auristatin E (MMAE)

Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent, which is linked to a monoclonal antibody (MAB). It is also a microtubule-disrupting agent .

S4114

Triclabendazole

Triclabendazole (CGA-89317) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.

S3970

Vindoline

Vindoline is a chemical precursor to vinblastine and exhibits antimitotic activity by inhibiting microtubule assembly.

S8789

SSE15206

SSE15206 is a tubulin polymerization inhibitor that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents.

S7787

Docetaxel Trihydrate

Docetaxel (RP56976, NSC 628503), an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

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.

S7783

Combretastatin A4

Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3.

S2284

Colchicine

Colchicine (Colchineos, Colchisol, Colcin) is a microtubule polymerization inhibitor with an IC50 of 3 nM.

S4071

Griseofulvin

Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.

S7762

TRx0237 (LMTX) mesylate

TRx 0237 (LMTX™) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.

S7497

CK-636

CK-636 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.

S3725

ELR-510444

ELR-510444 is a novel microtubule disruptor with potential antivascular effects and in vivo antitumor efficacy, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells.

S4269

Vinorelbine Tartrate

Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.

S7495

TAI-1

TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.

S7930

Ixabepilone (BMS-247550)

Ixabepilone (BMS-247550, Azaepothilone B, BMS 247550-1, Ixempra) is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis.

S4505

Vinblastine sulfate

Vinblastine sulfate (NSC49842) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.

S7493

INH1

INH1 is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.

S7494

INH6

INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.

S4535

Methylene Blue

Methylene Blue is used as a dye in chromoendoscopy. It Inhibits tau filament formation with IC50 of 1.9μM. Also it inhibits soluble guanylyl cyclase.

S5919

KHS101 hydrochloride

KHS101 is a small-molecule inhibitor of TACC3, which is a key component of centrosome-microtubule dynamic networks.

Catalog No. Information Product Use Citations Product Validations
S1233

2-Methoxyestradiol (2-MeOE2)

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

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.

Tags: microtubule inhibition | microtubule drugs | microtubule cancer | microtubule assay | microtubule phosphorylation | tubulin pathway | microtubule poison | microtubule inhibitors cancer | microtubule inhibitor drugs | microtubule inhibitor review