microtubule associated

Microtubule-associated protein tau (26-44) is a synthetic peptide with an amino group conjugated to glutamine and a carboxyl group conjugated to lysine.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Maytansinol (Ansamitocin P-0) inhibits microtubule assembly and causes microtubule disassembly in vitro.

Ixabepilone (Azaepothilone 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.

CCB02 is a selective CPAP-tubulin interaction inhibitor (IC50: 689 nM) with anti-tumor activity, showing no inhibition on cell cycle- and centrosome-related kinases, nor affecting the phosphorylation status of Aurora-A, CDK2, Plk1, Plk2, and CHK1.

Cevipabulin (TTI-237) is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).

Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

OSIP-486823(CP248) is a novel and potent microtubule disruptor with affinity for both protein kinase G (PKG) and microtubules.

Ombrabulin hydrochloride is a synthetic, selective CA-4 phosphate ester or derivative of Ombrabulin to disrupt the tubulin cytoskeleton of endothelial cells and has antivascular effects. Ombrabulin is a tubulin polymerizing inhibitor, a member of the combretastatin A-4 compound class, which is a water-soluble tubulin depolymerizing tumor vascularizing compound.

Sabizabulin (ABI-231) is a potent, orally bioavailable α- and β-tubulin inhibitor that is active against melanoma and prostate cancer cell lines. Sabizabulin inhibits tumor growth and metastatic phenotypes of cervical cancer cells by targeting HPV E6 and E7 and is also being studied in prostate cancer.

CID-663143 inhibits cancer cell growth and shows microtubule-binding activity.

Erbulozole (R 55104) is a potent synthetic microtubule inhibitor with anti-invasive, anti-tumor, and radiosensitizing activities that induces Wernicke's encephalopathy-like neurotoxicity.

AK301 is a potent and selective inhibitor of tubulin polymerization and an effective sensitizer of cancer cells to apoptotic ligands (EC50 < 200 nM). Colon cancer cells arrested in mitosis with AK301 readily underwent a p53-dependent apoptosis following compound withdrawal and arrest release.

Sabeluzole (R-58735) has antiepileptic and cognitive enhancing effects, inhibits neurotoxin-induced tau expression and cell death.Sabeluzole is protective against chlordiazepoxide-induced habituation disorders and may be useful in the study of Alzheimer's disease.

Suprafenacine (N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide) is a cell-permeable microtubule destabilizer that induces cell cycle arrest and apoptosis in G2/M phase. Suprafenacine binds to microtubules and inhibits aggregation at the colchicine junction. Suprafenacine is selective for cancer cells, including drug-resistant cancer cells.

L-Clausenamide is an alkaloid extracted from the leaves of the yellow bark (Clausena lansium (Lour) skeels) and can be used to improve cognitive function. L-Clausenamide inhibits beta-amyloid (Aβ) toxicity and prevents the formation of neurofibrillary tangles by inhibiting tau phosphorylation. L-Clausenamide has neuroprotective activity and can be used to modulate stimuli triggered by Aβ25-35. L-Clausenamide can be used to study neurological disorders like Alzheimer's disease.

cis-trismethoxy Resveratrol ((Z)-3,5,4'-Trimethoxystilbene) inhibits tubulin polymerization (IC50 = 4 μM) and has anti-mitotic effects.

ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

LY3372689 (Formulaic Ia) is an oral, highly selective, CNS-permeable O-GlcNAcase (OGA) inhibitor. LY3372689 exerts a neuroprotective effect by inhibiting OGA enzymatic activity, increasing the O-GlcNAc glycosylation level of tau protein, and thereby reducing abnormal tau phosphorylation and the formation of neurofibrillary tangles. LY3372689 can be used in research on tau-related diseases, including Alzheimer’s disease.

C004019 belongs to PROTACs and is a tau protein-targeted degrader (via recruitment of VHL E3 ligase) with blood-brain barrier permeability and selective tau degradation capability. This compound significantly reduces tau levels and improves cognitive function, and is used in research on Alzheimer's disease and related tauopathies.

Terflavoxate is a novel, orally active, semisynthetic statin microtubule inhibitor commonly used in combination with capecitabine. Terflavoxate is used in cancer research.

T-900607 is a novel microtubule protein active agent that disrupts microtubule polymerization through a unique mechanism of action. t-900607 is cardiotoxic.

Cemadotin free base(LU103793 free base) is a novel anti-limiting peptide , an analog of Dolastatin 15, a naturally occurring cytotoxic peptide that blocks mitosis and inhibits microtubules (tubulin) with a Ki of 1 μM. Cemadotin is used in research against cancer.

AC 7739 is a microtubule protein binding agent with anticancer and antitumor activity that inhibits advanced solid tumors and in situ transplanted tumors.