(-)-Blebbistatin is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.

RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models.

PLN-1474 (compound 1) is an orally active and selective avß1 integrin inhibitor with an IC50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder.

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.

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.

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.

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.

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.

K34c is a potent and selective α5β1 integrin antagonist. K34c can be used for glioblastoma research.

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

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.

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.

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.

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.

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.

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.

Kolavenic acid analog (KAA) is an anticancer agent. Kolavenic acid analog shows strong activity against HSET-overproducing yeast cells. Kolavenic acid analog inhibits centrosome clustering in human cancer cells containing high HSET levels and supernumerary centrosomes.

BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1), with a Ki of 25.8 nM. BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders.

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.

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.

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

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.

SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E.

Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.

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.

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.

PF-2771 is a potent, selective CENP-E inhibitor with IC50 of 16.1 nM; does not inhibit the ATPase activities of highly related kinesins (Eg5/KSP, chromokinesin and MCAK, IC50> 1 uM); selectively inhibits proliferation of basal breast cancer cell lines; regresses tumor growth correlated with increased phospho-HH3-Ser10 levels in a breast cancer xenograft tumor model.

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.

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.

KIF18A inhibitor 24 is a highly potent, in vivo active inhibitor of mitotic kinesin KIF18A with IC50 of 61 nM.KIF18A inhibitor 24 binds at the interface of KIF18A and tubulin.KIF18A inhibitor 24 exhibits significant mitotic arrest in MDA-MB-157 mitotic cells with EC50 of 11 nM, followed by cell death either in mitosis or in the subsequent interphase, which is sustained for 24 h.