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colchicine site

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35

Inhibitors & Agonists

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Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-155362
    Tubulin polymerization-IN-56

    		Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-56 (compound 8l), an indazole derivative, is a potent tubulin polymerization inhibitor through interacting with the colchicine site, resulting in cell cycle arrest and cellular apoptosis. polymerization-IN-56 reduces cell migration and leads to more potent inhibition of tumor growth in vivo .
    Tubulin polymerization-IN-56
  • HY-150761
    MY-875

    		Microtubule/Tubulin Apoptosis Cancer
    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 .
    MY-875
  • HY-162089
    MY-1442

    		Microtubule/Tubulin Apoptosis Cancer
    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 .
    MY-1442
  • HY-149020
    Tubulin polymerization-IN-26

    		Microtubule/Tubulin Apoptosis Cancer
    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 .
    Tubulin polymerization-IN-26
  • HY-155139
    Tubulin polymerization-IN-45

    		Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-45, a tubulin-targeting agent, is a tubulin polymerization inhibitor. Tubulin polymerization-IN-45 binds to the colchicine site of tubulin. Tubulin polymerization-IN-45 induces apoptotic cell death in hepatocellular cancer (HCC) cells .
    Tubulin polymerization-IN-45
  • HY-149414
    MY-673

    		Microtubule/Tubulin Apoptosis ERK TGF-beta/Smad Cancer
    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 .
    MY-673
  • HY-156737
    Tubulin polymerization-IN-49

    		Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-49 (compound 12d) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-49 bound to colchicine site on tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-49 induces cell cycle arrest at G2/M phase and apoptosis. Tubulin polymerization-IN-49 has anticancer active and prevents tumor generation, inhibits tumor proliferation and angiogenesis .
    Tubulin polymerization-IN-49
  • HY-147947
    Tubulin polymerization-IN-30

    		Microtubule/Tubulin Cancer
    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 .
    Tubulin polymerization-IN-30
  • HY-151397
    Tubulin polymerization-IN-36

    		Microtubule/Tubulin Cancer
    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 .
    Tubulin polymerization-IN-36
  • HY-151398
    Tubulin polymerization-IN-37

    		Microtubule/Tubulin Cancer
    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 .
    Tubulin polymerization-IN-37
  • HY-152156
    Tubulin inhibitor 11

    		Microtubule/Tubulin Apoptosis Cancer
    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 .
    Tubulin inhibitor 11
  • HY-157543
    Tubulin polymerization-IN-59

    		Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-59 ((R)-9k) is a potent inhibitor of colchicine binding site inhibitor (CBSI). Tubulin polymerization-IN-59 inhibits tubulin polymerization .
    Tubulin polymerization-IN-59
  • HY-163270
    PM534

    		Microtubule/Tubulin Cancer
    PM534, tubulin targeting agent, inhibits tubulin assembly with IC50 values of 0.8-3.2 nM. PM534 binds to the colchicine site of tubulin, which has high antitumor activity .
    PM534
  • HY-106825
    Clanfenur

    		Microtubule/Tubulin Cancer
    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 .
    Clanfenur
  • HY-151982
    Tubulin polymerization-IN-39

    		Microtubule/Tubulin Cardiovascular Disease Cancer
    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 .
    Tubulin polymerization-IN-39
  • HY-137974
    8-Epixanthatin

    		STAT Apoptosis Cancer
    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 .
    8-Epixanthatin
  • HY-106423
    Mivobulin

    NSC 613862; (S)-(-)-NSC 613862

    		 Microtubule/Tubulin Cancer
    Mivobulin (NSC 613862) is a tubulin inhibitor, binds to tubulin in the region that overlaps the colchicine site, and inhibits tubulin polymerization. Mivobulin (NSC 613862) promotes the formation of abnormal polymers and a GTPase activity in the tubulin dimer. Anti-cancer activity .
    Mivobulin
  • HY-152143
    Tubulin polymerization-IN-41

    		Microtubule/Tubulin Apoptosis Cancer
    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 .
    Tubulin polymerization-IN-41
  • HY-118748
    Suprafenacine

    SRF

    		 Microtubule/Tubulin Cancer
    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 .
    Suprafenacine
  • HY-121524
    DJ101

    		Microtubule/Tubulin Cancer
    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 .
    DJ101
  • HY-14444
    Plinabulin

    NPI-2358

    		 Microtubule/Tubulin Cancer
    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 .
    Plinabulin
  • HY-163356
    Tubulin polymerization-IN-60

    		Microtubule/Tubulin Apoptosis Cancer
    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 .
    Tubulin polymerization-IN-60
  • HY-119427
    Anti-melanoma agent 3

    		Others Cancer
    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 .
    Anti-melanoma agent 3
  • HY-106008
    Avanbulin

    BAL27862

    		 Microtubule/Tubulin Cancer
    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 .
    Avanbulin
  • HY-147888
    Tubulin inhibitor 29

    		Microtubule/Tubulin Cancer
    Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site .
    Tubulin inhibitor 29
  • HY-121993
    Combretastatin A-1

    		Microtubule/Tubulin Cancer
    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 .
    Combretastatin A-1
  • HY-149363
    Tubulin polymerization-IN-43

    		Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-43 (compound 15h) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-43 disrupts cellular microtubule networks by targeting the Colchicine (HY-16569) site, and promots cell cycle arrest of leukemia cells at G2/M phase and cell apoptosis, as well as inhibiting angiogenesis .
    Tubulin polymerization-IN-43
  • HY-162227
    Antitumor agent-138

    		Microtubule/Tubulin Apoptosis Cancer
    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 .
    Antitumor agent-138
  • HY-16146
    Combretastatin A-1 phosphate tetrasodium

    OXi-4503 tetrasodium

    		 Microtubule/Tubulin Cancer
    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 .
    Combretastatin A-1 phosphate tetrasodium
  • HY-143251
    Tubulin inhibitor 13

    		Microtubule/Tubulin Apoptosis Cancer
    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 .
    Tubulin inhibitor 13
  • HY-149374
    Tubulin inhibitor 36

    		Microtubule/Tubulin Cancer
    Tubulin inhibitor 36 (Compound 10) is a novel and potent tubulin inhibitor and inhibits the polymerization of microtubular protein then induces apoptosis with an IC50 value of 1.5±0.1 μM. Tubulin inhibitor 36 (Compound 10) has significant anti-mitotic effect and exhibits activities against glioblastoma cells. Tubulin inhibitor 36 (Compound 10) has anti-tumor effects and can be used for glioblastoma multiforme (GBM) research .
    Tubulin inhibitor 36
  • HY-161324
    Tubulin degrader 1

    		Microtubule/Tubulin Cancer
    Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
    Tubulin degrader 1
  • HY-148265
    Antiproliferative agent-14

    		Microtubule/Tubulin Cancer
    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 .
    Antiproliferative agent-14
  • HY-13270
    ABT-751

    E7010

    		 Microtubule/Tubulin Autophagy Apoptosis Cancer
    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 .
    ABT-751
  • HY-162319
    Tubulin/HDAC-IN-4

    		Apoptosis HDAC Microtubule/Tubulin Reactive Oxygen Species Cancer
    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 .
    Tubulin/HDAC-IN-4

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