>98%,Standard References

>98%,Standard References

>98%,Standard References

A novel microtubule inhibitor, downregulates T315I mutant Bcr-Abl and induces apoptosis of imatinib-resistant chronic myeloid leukemia cells.

A novel microtubule targeting agent that induces apoptosis, upregulates death receptors, and potentiates TRAIL-mediated apoptosis in multiple cancer cells.

A novel tubulin inhibitor that inhibits the proliferation of cancer cell lines with IC50 of 0.2-1.0 uM.

ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.

Cabazitaxel (Jevtana, XRP6258) is a semi-synthetic derivative of a natural taxoid.

CKD-516 (Valecobulin, CKD516) is a potent beta-tubulin polymerization inhibitor with marked antitumor activity both in vitro and in vivo.

CYT997 is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. Phase 1/2.

DZ-2384 (DZ2384) is a microtubule-targeting agent, exhibits potent antitumor activity in models of multiple cancer types.

Epothilone B is a Taxol-like microtubule-stabilizing agent with EC0.01 of 1.8 μM.

Eribulin is an anticancer drug marketed by Eisai Co. under the trade name Halaven. Eribulin is also known as E7389 and ER-086526, and also carries the US NCI designation NSC-707389. It is used to treat certain patients with breast cancer and liposarcoma.

Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.

Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.

Ixabepilone (Azaepothilone B; BMS 247550) is an epothilone B analog and nontaxane microtubule-stabilizing compound with clinical activity in a range of solid tumors.

MP-HJ-1b is a novel potent inhibitor of microtubule and tumor cell growth, binds the colchicine pocket at the intra-dimer interface, depolymerizes microtubules and affects spindle formation.

Ombrabulin (AVE8062) hydrochloride is a synthetic derivative of CA-4-P, which inhibits growth in a large number of drug-resistant animal tumors and carcinogen-induced tumors.

Plocabulin (PM060184) is a novel tubulin-binding agent binding to αβ-tubulin dimer with nanomolar affinity, inhibits a panel of 23 tumor cell lines with GI50 of 20 pM-5 nM.

VERU-111 (Sabizabulin) is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities. Sabizabulin is a novel oral agent with both anti-viral and anti-inflammatory activities.Sabizabulin is a cytoskeleton disruptor which by causing microtubule depolymerization has both anti-viral and anti-inflammatory activity and could be effective against the SARS-CoV-2 virus by disrupting its intracellular transport along the microtubules. Microtubule trafficking is critical for viruses to be transported, replicated, assembled, and released from the cell. In addition, microtubule depolymerization drugs that target the “colchicine binding site” of microtubules, like sabizabulin, also have strong anti-inflammatory effects, including the potential to treat the cytokine release syndrome (cytokine storm) and septic shock induced by the SARS-CoV-2 viral infection that is associated with high COVID-19 mortality rates.

VERU-111 analogue 13f is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities.

Vinorelbine (Navelbine) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.

Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induce apoptotic cell death. Batabulin has efficacy against multidrug-resistant (MDR) tumors.

Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.

MAP4343 is the 3-methylether derivative of Pregnenolone. MAP4343 binds in vitro to microtubule-associated protein 2 (MAP2), stimulates the polymerization of tubulin, enhances the extension of neurites and protects neurons against neurotoxic agents.

Curvulin, isolated from Curvularia lunata, is a phytotoxin. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.

Batabulin sodium (T138067 sodium) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin sodium affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.

Cryptophycin 1 is a potent cytotoxic antimicrotubule agent which is isolated from Nostoc sp. Cryptophycin 1 can induce cells apoptosis, and exhibits antitumor activity and exceptional antiproliferative potency.

Docetaxal (10-Acetyl docetaxel; PNU-101383), an analog of Docetaxel, is a microtubule disassembly inhibitor, with antimitotic activity. Docetaxal has cytotoxicity for murine leukemic cells.

Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (?-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.

Podophyllotoxone is isolated from the roots of Dysosma versipellis and has anti-cancer activities.Podophyllotoxone is able to inhibit the tubulin polymerization.

Vc-MMAD consists the ADCs linker (Val-Cit) and potent tubulin (MMAD). Vc-MMAD is a drug-linker conjugate for ADC.

Bis-ANS dipotassium is a fluorescent probe of hydrophobic protein. Bis-ANS binds to tubulin with a Kd of 2 μM. Bis-ANS dipotassium is a potent biphasic modulator of protein liquid-liquid phase separation (LLPS). Bis-ANS dipotassium promotes LLPS at low concentrations but suppresses LLPS at high concentrations.

Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.

Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.

Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects.

20-O-Demethyl-AP3 is a minor metabolite of Ansamitocin P-3. Ansamitocin P-3, a microtubule inhibitor, is a macrocyclic antitumor antibiotic.

Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects.

Paclitaxel D5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization.

PF-06380101 D8 (Aur0101 D8) is a deuterium labeled PF-06380101. PF-06380101, an Auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue.

MC-betaglucuronide-MMAE-2 is a drug-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.

MC-VC-PAB-MMAD is a drug-linker conjugate for ADC with potent antitumor activity by using MMAD (a potent tubulin inhibitor), linked via the cleavable ADC linker MC-VC-PAB.

OSu-Glu-VC-PAB-MMAD is a drug-linker conjugate for ADC with potent antitumor activity by using MMAD (a potent tubulin inhibitor), linked via the cleavable ADC linker OSu-Glu-VC-PAB.

AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC.

Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity.

Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC.

Amiprofos methyl (BAY-NTN 6867) is a phosphoric amide herbicide. Amiprofos methyl is a specific and potent antimicrotubule agent. Amiprofos methyl directly poisons microtubule dynamics in plant cells.

Sovilnesib(AMG650) is a kinesin-like protein KIF18A inhibitor (WO2020132648). Sovilnesib can be used for the research of cancer.

Violanone, an isoflavanone compound, can inhibit tubulin polymerization. Violanone also exhibits larvicidal activity against A. aegypti.

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

Dolastatinol is a synthetic analog of dolastatin 10 and low nanomolar inhibitor of tubulin polymerization.

PF-06380101 D8 (Aur0101 D8) is a deuterium labeled PF-06380101. PF-06380101, an Auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue.

Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.

DHA-paclitaxel is an inert prodrug composed of the natural fatty acid DHA covalently linked to the C2'-position of paclitaxel. The paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Compared to Paclitaxel, DHA-Paclitaxel targets tumor cells more specifically because tumor cells absorb large amounts of natural fatty acids for use as biochemical precursors and energy sources.

Tesetaxel is a orally active, semisynthetic microtubule inhibitor of the taxane class for the treatment of cancer, including colorectal and gastric cancer.

Cis-trismethoxy resveratrol is a potent anti-mitotic reagent.Cis-trismethoxy resveratrol inhibits tubulin polymerization with an IC50 value of 4 μM.

Verubulin hydrochloride(MPC 6827 hydrochloride) is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals.

LG308 is a novel synthetic compound with antimicrotubule activity. LG308 induces mitotic phase arrest and inhibits G2/M progression significantly which is associated with the upregulation of cyclin B1 and mitotic marker MPM-2 and the dephosphorylation of cdc2. LG308 also induces apoptosis and cell death. LG308 significantly suppresses tumor growth. LG308 with antimitotic activity has the potential for the research of prostate cancer.

(R)-AM-5308 is a potent kinesin KIF18A inhibitor (WO2021211549A1, C13).

(S)-AM-5308 (compound 7-13) is a potent kinesin KIF18A inhibitor with an IC50 of 46 nM for KIF18A ATPase. (S)-AM-5308 has the potential for cancer research.

SB-216 is a potent tubulin polymerization inhibitor. SB-216 shows strong antiproliferative potency in a panel of human cancer cell lines, including melanoma, lung cancer, and breast cancer.  SB-216 can be used for cancer research.

OXi8007 is a water-soluble phosphate prodrug of OXi8006, a tubulin-binding compound.

2-Methoxyestradiol-13C6 (2-ME2-13C6) is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.

Microtubule destabilizing agent-1 (Compound 12b) acts as a microtubule destabilizing agent (MDA) based on hydroxamic acid, could serve as a potential MDA for further investigation. Microtubule destabilizing agent-1 shows favorable metabolism stability, high bioavailability, and potent antitumor activity.

AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors.

Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.

A small molecule that inhibits tubulin polymerization.

IMB5476 (IMB 5476) is a nitrobenzoate microtubule inhibitor, exerts broad-spectrum cytotoxicity against various human tumor cell lines (NCI-H460, IC50=144 nM).IMB5476 inhibits purified tubulin polymerization in vitro, binds to tubulin at the colchicine pocket.IMB5476 induced cell death by mitotic catastrophe and apoptosis, disrupted microtubule networks in cells and arrested cell cycle at G2/M phase.IMB5476 is a poor substrate of P-glycoprotein and exhibited potent cytotoxicity against drug-resistant tumor cells.IMB5476 inhibited angiogenesis in vitro, also inhibited the growth of drug-resistant KBV200 xenografts in mice.

Microtubule inhibitor PP-13 is a novel microtubule-destabilizing agent, directly inhibits microtubule assembly by targeting the colchicine-binding site in β-tubulin.PP-13 inhibits the growth of a wide range of cancer cell types, including targeted therapy-resistant and multidrug-resistant (MDR) cell lines (IC50=76-255 nM).PP-13 overcomes the multidrug-resistant (MDR) phenotype in cancer cells, induces mitotic blockade in cancer cells, interferes with both mitotic microtubule organization and spindle pole integrity.PP-13 induces cell prometaphase arrest then asymmetric division or direct apoptotic death.PP-13 reduces tumour growth and metastasis invasion in vivo.

PCH-1 is a potent antitumor agent that disrupts microtubule assembly, leading to cancer cell death, interacts vinblastine binding site on tubulin; PCH-1 exhibits the strongest cytotoxic activity through interaction with tubulin, leading to cell cycle arrest and induction of apoptosis. PCH-1 efficiently inhibits the growth of NSCLC cancer cell lines at micromolar concentrations (A-549 IC50=4.32 uM, H226 IC50=4.69 uM), and non-toxic to normal cells.

PST-3 (Microtubule inhibitor PST-3) is a novel microtubule inhibitor exhibited broad-spectrum cellular cytotoxicity and in vivo potency with high safety.PST-3 inhibits different cancer cell with high safety (BT549 IC50=15 uM, MDA-MB-468 IC50=16 uM), inhibits human breast cancer cell clonogenic growth with IC50 values rang from 3 uM to 25 uM (MDA-MB-231 cell IC50=11.43 uM).PST-3 binds to the colchicine binding site on microtubule, induces morphological changes, disrupts the structure of microtubule in cells and inhibits tubulin polymerization, arrests BT549 and MDA-MB-468 cells in G2/M phase.PST-3 shows preferential growth inhibition in triple-negative breast cancer xenografts growth without neurotoxicity in vivo.

Todalam is a novel small molecule tubulin inhibitor with IC50 of 8.8 uM against HeLa cells, fully inhibits microtubule formation with IC50 of 48 uM, acting as a reversible microtubule-destabilizing agent in vitro and in cells.Todalam kills different type of mammalian cells, induces G2/M arrest, disrupts cellular microtubule networks, and can inhibit cell growth in a synergistic manner in combination with vinblastine.Todalam achieves its effect by locking α-tubulin in an inactive conformational state and by sequestering tubulin dimers.Todalam is the first-ever, fully rationally designed tubulin inhibitor with an original molecular mechanism of action.

THK-5117, an arylquinoline derivative, displays high binding affinity to tau fibrils with a Ki of 10.5 nM. THK-5117 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD)  brain homogenates. 18F-THK-5117 has the potential to act as a tau imaging PET probe.

isoCA-4, a Combretastatin A4 derivative, is a tubulin polymerization inhibitor. isoCA-4 has anti-proliferative activities.

THK-5105, an arylquinoline derivative, displays high binding affinity to tau fibrils. THK-5105 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD)  brain homogenates. 18F-THK-5105 has the potential to act as a tau imaging PET probe.

IQTub4P is a potent microtubule (MT) inhibitor. IQTub4P has the cytotoxicity in in HeLa cells, with EC50 of 170 nM. IQTub4P inhibits microtubule structure and function. IQTub4P is well-tolerated in vivo.

HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer.

Vindesine sulfate is a potent tubulin inhibitor with an Ki of 0.110 µM. Vindesine sulfate shows anti-proliferation effect in vitro. Vindesine sulfate shows antitumor effect in vivo.

SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs.

Oryzalin is a dinitroaniline herbicide, binding to plant tubulin and inhibits microtubule (MT) polymerization in vitro. Oryzalin depolymerizes MTs and prevented the polymerization of new MTs at all stages of the mitotic cycle.

Eleutherobin is a potent β-microtubule inhibitor with an IC50 value of 2 μM. Eleutherobin can be isolated from a marine soft coral. Eleutherobin has cytotoxic activity against cancer cells with similar potency to that of Paclitaxel. Anticancer activity.

Epothilone E is a related compound of epothilone, which inhibits microtubule protein function and blocks cell division, and has anti-tumor activity.

MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity.

Tubulin polymerization-IN-2 is a potent anticancer agent targeting to β-tubulin with an IC50 value of 0.92 μM. Tubulin polymerization-IN-2 shows promising activity against various leukemia, non-small lung, renal, prostate, and breast cancer cell lines.

TAM470 is a novel cytolysin, inhibiting tubulin polymerization and microtubule depolymerization. TAM470 can be used in the synthesis of OMTX705 as payload molecule, OMTX705 is a novel FAP-targeting antibody-drug conjugates (ADCs) with antitumor activity.

Cemadotin (LU103793) is an analogue of Dolastatin 15 which is naturally occurring cytotoxic peptides. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer.

ALM201 is a small 23 amino acid peptide derived from the FK506 binding protein FKBPL, a targeted microtubule binding agent which exhibits potent anti-angiogenic activity in vitro and in vivo.

CH-2-77 is a potent colchicine-binding site inhibitor (CBSI) targeting tubulin, shows potent anti-proliferative activity against a panel of cancer cells in vitro and efficacious anti-tumor effects in vivo.

CH-2-77 analogue 60c is a potent colchicine-binding site tubulin inhibitor, inhibits tubulin polymerization and is effective against P-glycoprotein-mediated multiple drug resistance and taxol resistance.

EAPB02303 (EAPB 02303) is a novel microtubule-disrupting agent with in-vivo activity in PDAC and in-vitro synergy with Paclitaxel, inhibits A375 melanoma cell line with IC50 of 3 nM.

FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells.

KGP591 is a small molecule inhibitor of tubulin polymerization with IC50 of 0.57 uM, exhibits cytotoxicity against the MCF-7 and MDA-MB-231 human breast cancer cell lines with GI50 of 320 and 102 nM, respectively.

KGP618 is the phosphate prodrug salt of KGP591, which is a small molecule inhibitor of tubulin polymerization with IC50 of 0.57 uM.

An orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo.

R-huezole is a phase-separating small molecule that forms liquid droplets to selectively sequester tubulin, enters cultured human cells and prevents cell mitosis by forming tubulin-concentrating condensates in cells.

TN-2 is a potent, dual tubulin/NRP1-targeting inhibitor with IC50 of 0.71 uM (tubulin polymerization) and 0.85 uM (NRP-1), inhibits proliferation and angiogenesis of tumor cells.