Microtubule Associated

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S1150

Paclitaxel

Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.

S1148

Docetaxel

Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

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.

S1364

Epothilone B (EPO906, Patupilone)

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

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.

S7762New

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.

S7930New

Ixabepilone (BMS-247550)

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.

S4505New

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.

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.

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.

S1248

Vinblastine

Vinblastine 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.

S2195

CYT997 (Lexibulin)

CYT997 (Lexibulin) 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. Phase 3.

S1640

Albendazole

Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.

S2209

Vinflunine Tartrate

Vinflunine is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity. Phase 3.

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 is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.

S4114

Triclabendazole

Triclabendazole is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.

S7787

Docetaxel Trihydrate

Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

S7783

Combretastatin A4

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

S4071

Griseofulvin

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

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.

S4269

Vinorelbine Tartrate

Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin.

S7495

TAI-1

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

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.

Catalog No. Information Product Use Citations Product Validations
S1150

Paclitaxel

Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.

S1148

Docetaxel

Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

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.

S1364

Epothilone B (EPO906, Patupilone)

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

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.

S7762New

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.

S7930New

Ixabepilone (BMS-247550)

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.

S4505New

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.

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.

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.

S1248

Vinblastine

Vinblastine 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.

S2195

CYT997 (Lexibulin)

CYT997 (Lexibulin) 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. Phase 3.

S1640

Albendazole

Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.

S2209

Vinflunine Tartrate

Vinflunine is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity. Phase 3.

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 is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.

S4114

Triclabendazole

Triclabendazole is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.

S7787

Docetaxel Trihydrate

Docetaxel, an analog of paclitaxel, is an inhibitor of depolymerisation of microtubules by binding to stabilized microtubules.

S7783

Combretastatin A4

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

S4071

Griseofulvin

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

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.

S4269

Vinorelbine Tartrate

Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin.

S7495

TAI-1

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

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.

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