Search Result
Results for "
colchicine binding sites
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-150761
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Microtubule/Tubulin
Apoptosis
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Cancer
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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 .
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- HY-162089
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Microtubule/Tubulin
Apoptosis
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Cancer
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MY-1442 (I-3) is a microtubulin polymerization inhibitor. MY-875 inhibits tubulin polymerization by targeting colchicine binding sites. MY-1442 has anticancer activity. MY-1442 can induce apoptosis of MGC-803 cells and inhibit cell migration .
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- HY-149414
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Microtubule/Tubulin
Apoptosis
ERK
TGF-beta/Smad
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Cancer
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MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro .
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- HY-157543
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-59 ((R)-9k) is a potent inhibitor of colchicine binding site inhibitor (CBSI). Tubulin polymerization-IN-59 inhibits tubulin polymerization .
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- HY-152156
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
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- HY-149020
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-26 (compound 12h) can inhibit the polymerization of microtubulin by binding to the colchicine binding site of microtubulin with an IC50 value of 4.64 μM. Tubulin polymerization-IN-26 can induce apoptosis and inhibit cell metastasis or migration, and can be used as a potential compound for lung cancer research .
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- HY-147947
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM .
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- HY-170864
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- HY-151398
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-37 is a tubulin polymerization inhibitor (IC50: 2.3 μΜ). Tubulin polymerization-IN-37 binds to the colchicine site of tubulin and inhibits colchicine binding. Tubulin polymerization-IN-37 can be used in the research of cancers, such as lymphomas .
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- HY-151397
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-36 is a tubulin polymerization inhibitor (IC50: 2.8 μΜ). Tubulin polymerization-IN-36 binds to the colchicine site of tubulin and inhibits colchicine binding. Tubulin polymerization-IN-36 can be used in the research of cancers, such as lymphomas .
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- HY-106825
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Microtubule/Tubulin
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Cancer
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Clanfenur is a substituted benzoylphenylurea, an analogue of the pesticide fenfluramide, with potential antineoplastic activity. Clanfenur can bind to the colchicine-binding site on β-tubulin, inhibit microtubule polymerization, and thus prevent tumor cell replication .
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- HY-162594
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Microtubule/Tubulin
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Cancer
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Antitumor agent-164 (compound 60c) is a colchicine-binding site inhibitor (CBSI) with potency against taxane-sensitive TNBC. Antitumor agent-164 is a next-generation derivative of VERU-111 .
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- HY-151982
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Microtubule/Tubulin
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Cardiovascular Disease
Cancer
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Tubulin polymerization-IN-39 is a tubulin polymerization inhibitor (IC50: 4.9 μM). Tubulin polymerization-IN-39 occupies the colchicine-binding site. Tubulin polymerization-IN-39 inhibits cancer cell proliferation .
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- HY-137974
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STAT
Apoptosis
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Cancer
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8-Epixanthatin is a potential colchicine binding site inhibitor isolated from Xanthium chinese Mill. 8-Epixanthatin can inhibit the activation of STAT3, induce apoptosis, and has anti-tumor activity .
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- HY-152143
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-41 is a potent tubulin polymerization inhibitor with the IC50 of 2.61 μM. Tubulin polymerization-IN-41 targets the Colchicine-binding site of tubulin. Tubulin polymerization-IN-41 has anticancer effects .
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- HY-119361
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(Rac)-Deoxysappanone B 7,4' dimethyl ether
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Microtubule/Tubulin
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Cancer
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(Rac)-Deox B 7,4, a homoisoflavanoid compound, inhibits microtubule polymerization via binding near the colchicine site and promote reversible G2 arrest. (Rac)-Deox B 7,4 possesses nanomolar anti-leukemic activity .
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- HY-118748
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SRF
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Microtubule/Tubulin
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Cancer
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Suprafenacine is a cell permeable, tubulin-destabilizing molecule which bind microtubules at the colchicine-binding site and inhibit polymerization. Suprafenacine can induce G2/M cell cycle arrest and apoptosis, and can be used for cancer research .
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- HY-121524
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Microtubule/Tubulin
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Cancer
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DJ101 is a potent and metabolically stable tubulin inhibitor. DJ101 targets the colchicine binding site and overcomes taxane resistance. DJ101 also inhibits melanoma tumor growth and lung metastasis. DJ101 can be used for prostate cancer research .
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- HY-119427
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Microtubule/Tubulin
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Cancer
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Anti-melanoma agent 3 (compound 5cb) is a 2-aryl-4-benzoyl-imidazole (ABI) derivative and an inhibitor of melanoma xenogeneic tumors. Anti-melanoma agent 3 exerts anticancer activity by interacting with the colchicine binding site to inhibit tubulin polymerization .
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- HY-163356
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-60 (BF3) is a tubulin polymerization inhibitor with anticancer activity. Tubulin polymerization-IN-60 (BF3) belongs to the colchicine binding site inhibitors (CBSIs) and disturbs cell cycle progression leading to G2/M arrest and apoptosis .
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- HY-14444
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NPI-2358
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Microtubule/Tubulin
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Cancer
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Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells . Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells .
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- HY-106008
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BAL27862
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Microtubule/Tubulin
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Cancer
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Avanbulin (BAL27862) is a potent, Colchicine site-binding, tubulin assembly inhibitor. Avanbulin inhibits tubulin assembly at 37 °C with an IC50 of 1.4 μM. Avanbulin binds to tubulin with an apparent Kd value of 244 nM. Avanbulin can be used for the research of cancer and cell division .
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- HY-120599A
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VERU-111 hydrochloride; ABI-231 hydrochloride
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Microtubule/Tubulin
Apoptosis
HPV
Endogenous Metabolite
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Cancer
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Sabizabulin hydrochloride is a potent orally bioavailable microtubule inhibitor with activity that interacts with the colchicine binding site. Sabizabulin hydrochloride demonstrated significant inhibition of melanoma tumor growth with an average IC50 of 5.2 nM in melanoma and prostate cancer cell lines. Pharmacological screening of Sabizabulin hydrochloride shows it has a low risk of potential side effects .
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- HY-143251
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 13 (E27) is a potent tubulin inhibitor with an IC50 value of 16.1 μM for the tubulin polymerization inhibition. Tubulin inhibitor 13 inhibits migration and invasion of cancer cells, induces apoptosis and has anticancer activity .
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- HY-121993
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Microtubule/Tubulin
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Cancer
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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 .
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- HY-163523
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Microtubule/Tubulin
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Cancer
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PYRIB-SO 2 is a potent antimitotic agent. PYRIB-SO 2 shows antiproliferative activity and induces cell cycle arrest at G2/M phase. PYRIB-SO 2 reduces and disruptes microtubule structures. PYRIB-SO 2 binds to the colchicine-binding site (C-BS) of α, β-tubulin .
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- HY-170563
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-72 (Compound 4a4) is an anticancer agent that acts as a tubulin polymerization inhibitor. It inhibits tubulin polymerization by binding to the colchicine site, leading to cancer cell arrest in the G2/M phase and inducing their apoptosis (Apoptosis). Tubulin polymerization-IN-72 has an IC50 of 0.4-2.7 nM against cancer cells.
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- HY-124083
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Microtubule/Tubulin
Apoptosis
Caspase
Mitochondrial Metabolism
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Cancer
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MPT0B214 is a microtubule inhibitor that strongly binds to the colchicine binding site of tubulin, preventing tubulin polymerization. MPT0B214 induces apoptosis through a mitochondrial/caspase 9 dependent pathway and shows cytotoxicity across various human tumor cell lines. MPT0B214 can be used for cancer research .
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- HY-162227
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Microtubule/Tubulin
Apoptosis
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Cancer
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Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis .
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- HY-16146
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OXi-4503 tetrasodium
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Microtubule/Tubulin
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Cancer
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Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a proagent 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 .
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- HY-148265
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Microtubule/Tubulin
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Cancer
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Antiproliferative agent-14 (compound 3b) a potent tubulin polymerization inhibitor, with an IC50 of 3.41 μM. Antiproliferative agent-14 has excellent antiproliferative activity. Antiproliferative agent-14 possess the ability to arrest cells at G2/M phases of the cell cycle .
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- HY-173074
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Microtubule/Tubulin
MDM-2/p53
Apoptosis
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Cancer
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Microtubulin-IN-1 (Compound 8g) is the inhibitor for microtubulin that targets colchicine-binding site, disrupts the microtubulin integrity, and induces the upregulation of p53. Microtubulin-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for NCI-H460, BxPC-3 and HT-29 is 2.4, 1.6 and 2.07 nM, respectively), arrests the cell cycle at G2/M phase, and induces apoptosis in NCI-H460 .
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- HY-163692
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-64 (Compound 8a) is an inhibitor for tubulin polymerization by occupying the colchicine binding site of tubulin, with IC50 of 6.9 μM. Tubulin polymerization-IN-64 inhibits proliferations of cancer cells A549, HeLa, HCT116 and HT-29, with IC50s of 2.42, 10.33, 6.28, 5.33 μM, respectively. Tubulin polymerization-IN-64 arrests cell cycle at G2/M phase, induces apoptosis in A549 .
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- HY-168565
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Apoptosis
Microtubule/Tubulin
Reactive Oxygen Species
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Cancer
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Tubulin polymerization-IN-70 (compound Q19) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-70 shows antiproliferative activity. Tubulin polymerization-IN-70 target the colchicine binding site of tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-70 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-70 induces mitochondrial membrane potential decrease and increases the levels of reactive oxygen species (ROS). Tubulin polymerization-IN-70 shows antiangiogenic and anticancer activity .
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- HY-13270
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E7010
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Microtubule/Tubulin
Autophagy
Apoptosis
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Cancer
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ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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- HY-162319
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Apoptosis
HDAC
Microtubule/Tubulin
Reactive Oxygen Species
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Cancer
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Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity .
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- HY-159921
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Microtubule/Tubulin
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Cancer
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Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a palladium (Pd)-mediated tubulin polymerization inhibitor prodrug. Developed based on colchicine binding site inhibitors (CBSIs), it reduces toxicity and enhances targeted release properties. Compared to the parent compound, Tubulin Polymerization-IN-1 prodrug exhibited 68.3-fold lower cytotoxicity, which can be restored in situ in the presence of Pd resin. Mechanistic studies showed that its anticancer activity is consistent with CBSIs. In vivo, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth (63.2%) when activated by Pd resin. It holds promise for research in the field of anticancer therapy .
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- HY-13270A
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E7010 hydrochloride
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Microtubule/Tubulin
Autophagy
Apoptosis
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Cancer
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ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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- HY-161863
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Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
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Cancer
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Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC50 of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC50s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrial membrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice
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- HY-170924
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active Tubulin polymerization inhibitor. Tubulin polymerization-IN-76 inhibits Tubulin polymerization with an IC50 of 2.505 μM by acting on the colchicine binding site, thereby disrupting intracellular Microtubule networks and interfering with cell mitosis. Tubulin polymerization-IN-76 demonstrates exceptional efficacy against MGC-803 and HGC-27 cells with IC50s of 1.61 and 1.82 nM, respectively. Tubulin polymerization-IN-76 effectively inhibits the colony formation and cell migration activities, and induces G2/M phase cycle arrest and Apoptosis in MGC-803 and HGC-27 cells.Tubulin polymerization-IN-76 shows a broad-spectrum antiproliferative activity .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-137974
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Source classification
Plants
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STAT
Apoptosis
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8-Epixanthatin is a potential colchicine binding site inhibitor isolated from Xanthium chinese Mill. 8-Epixanthatin can inhibit the activation of STAT3, induce apoptosis, and has anti-tumor activity .
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Cat. No. |
Product Name |
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Classification |
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- HY-159921
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Alkynes
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Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a palladium (Pd)-mediated tubulin polymerization inhibitor prodrug. Developed based on colchicine binding site inhibitors (CBSIs), it reduces toxicity and enhances targeted release properties. Compared to the parent compound, Tubulin Polymerization-IN-1 prodrug exhibited 68.3-fold lower cytotoxicity, which can be restored in situ in the presence of Pd resin. Mechanistic studies showed that its anticancer activity is consistent with CBSIs. In vivo, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth (63.2%) when activated by Pd resin. It holds promise for research in the field of anticancer therapy .
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