Curvulin, isolated from Curvularia lunata, is a phytotoxin[1]. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.
Natalizumab is a recombinant, humanized monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses[1].
Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs)[1][2].
Dolastatin 10 is a potent antimitotic peptide, isolated from the marine mollusk Dolabela auricularia, that inhibits tubulin polymerization.
Epothilone F is a Microtubule/Tubulin-stabilizing agent with anti-tumor activity. Epothilone F inhibits the proliferation of breast cancer cells, non-small cell lung cancer cells, drug-resistant ovarian cancer cells[1].
REDV is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV can be used for the research of cell adhesion[1].
2-Methoxyestradiol is an angiogenesis inhibitor and apoptosis inducer with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules.
MMAF (Monomethylauristatin F) is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.
ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.
Tubulin polymerization-IN-28 (compound-4) is a microtubule protein polymerization inhibitor with highly selective anticancer activity. Tubulin polymerization-IN-28 can be activated by NQO1 and effectively release combretastatin A-4 to kill tumor cells. Tubulin polymerization-IN-28 can induce cell apoptosis and be used in anti-cancer research[1].
TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain[1].
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[1].
GSK 3008348 (hydrochloride) is a small molecule integrin αvβ6 antagonist, extracted from patent WO/2014154725A1, example 1. The affinity (pIC50) for the human - a 6 protein in the Fluorescence Polarisation Assay for GSK 3008348 (hydrochloride) is 8.1, whereas its affinity in the cell Adhesion Assays was for: ανβ6 (pIC50 = 8.4); ανβ3 (pIC50 = 6); ανβ5 (pIC50 = 6.9); ανβ8 (pIC50 = 7.7).
PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner[1].
Vinflunine ditartrate is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family. Vinflunine ditartrate has anti-angiogenic, vascular-disrupting and anti-metastatic activities. Vinflunine ditartrate can be used for the research of transitional cell carcinoma of the urothelial tract, non-small cell lung cancer, and carcinoma of the breast[1][2].
GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.
EAPB 02303 is a microtubule-disrupting agent and inhibitor. EAPB 02303 induces mitosis arrest and impairment of spindle assembly. Thus, EAPB 02303 induces apoptosis and exhibits antitumor activity. EAPB 02303 also exhibits a potent synergy with Paclitaxel (HY-B0015) at lower concentrations[1].
NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM)[1].
Lifitegrast is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
Taltobulin (HTI-286; SPA-110) is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.IC50 value:Target: tubulinin vitro: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure [1]. In all cell lines tested, HTI-286 was a potent inhibitor of proliferation and induced marked increases in apoptosis. Despite similar transcriptomic changes regarding cell death and cell cycle regulating genes after exposure to HTI-286 or docetaxel, array analysis revealed distinct molecular signatures for both compounds [2].in vivo: Intravenous administration of HTI-286 significantly inhibited tumor growth in vivo (rat allograft model) [1]. HTI-286 significantly inhibited growth of PC-3 and LNCaP xenografts and retained potency in PC-3dR tumors. Simultaneous castration plus HTI-286 therapy was superior to sequential treatment in the LNCaP model [2].
Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease[1][2].
OSU-T315 is an inhibitor of integrin-linked kinase (ILK) with an IC50 of 600 nM.
Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.
Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis[1].
Tilavonemab (ABBV-8E12) is a humanised anti-tau antibody that binds amino acids 25-30 near the N-terminal end of the tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates and reduces brain atrophy. Tilavonemab can be used in the study of Alzheimer's disease[1].
Vincristine (Leurocristine) is a microtubule-destabilizing agent (MDA). Vincristine (Leurocristine) binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine (Leurocristine) is used to treat hematologic cancers, such as leukemia and lymphoma, and childhood sarcomas[1][2].
A potent, highly selective α4β1 integrin antagonist with Kd of <10 pM; the rate of BIO7662 binding is dependent on the metal ion concentration; directly competes with VCAM-1, CS-1, and BIO1211 for binding to the integrin.
Mavacamten-d1 (MYK461-d1; SAR439152-d1) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
P34cdc2 Kinase Fragment is associated with the completion of DNA replication in yeast mitosis. P34cdc2 Kinase can phosphorylate mitogen-activated protein 2 (MAP2) to regulate microtubules polymerization in Xenopus oocytes meiosis[1][2].