microtubule inhibitor 2

Microtubule inhibitor 2 is a highly potent and selective microtubule inhibitor, which is orally active. It induces cell death via ferroptosis, and exhibits notable antitumor activity [1].

Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis.

Thiabendazole (2-(4-Thiazolyl)benzimidazole) is a benzimidazole derivative with anthelminthic property.

Docetaxel (RP-56976), a semi-synthetic analog of paclitaxel, is a microtubule depolymerization inhibitor (IC50=0.2 μM) that attenuates the effects of bcl-2 and bcl-xL gene expression and exhibits apoptosis-inducing, anti-tumor activity.

Ibuprofen (Advil) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes.

Benproperine phosphate (Pirexyl phosphate) is a cough suppressant.

CK-636 (CK-0944636), an Arp2 3 complex inhibitor, can inhibit actin polymerization induced by the human (IC50: 4 μM), fission yeast (IC50: 24 μM) and bovine (IC50: 32 μM) Arp2 3 complex, respectively.

CK-666 is a cell-permeable inhibitor of the actin-related protein Arp2 3 complex, binding to and stabilizing its inactive state, thereby preventing the movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) configuration.

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It contains the microtubule polymerization inhibitor DM1 as the active metabolite, which inhibits microtubule polymerization. It is commonly used in breast cancer research.

MARK-IN-2 is a potent inhibitor of microtubule affinity-regulating kinase (MARK) with an IC50 of 5 nM.

Dynarrestin is an inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells. It inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-depen

JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L.

VCP-Eribulin, an Eribulin-based drug for antibody conjugates[1], combines the VCP (ADCs linker) with Eribulin, a distinct microtubule inhibitor used in cancer treatments[2].

DPP-21 is an inhibitor of microtubule protein polymerization (IC50: 2.4 μM). It exhibits antiproliferative activity against various cancer cell lines, with IC50 values of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23), and 9.37 nM (HepG2). DPP-21 induces cell cycle arrest at the G2 M phase of mitosis and subsequently triggers apoptosis in tumor cells by decreasing Bcl-2 while increasing pro-apoptotic protein Bax levels.

EGFR VEGFR2-IN-1 (Compound 10e) serves as an inhibitor for VEGFR-2 and EGFR, with respective IC50 values of 0.26 and 0.14 μM. It inhibits microtubule protein polymerization with an IC50 of 40.9 μM and induces cell apoptosis (Apoptosis). EGFR VEGFR2-IN-1 is applicable in research related to anti-leukemia and anti-lymphoma treatments.

Sutopin-2 is a topoisomerase II inhibitor that affects cell cycle progression and microtubule stability. It induces cell cycle arrest by regulating the nuclear-cytoplasmic transport of cyclin B1.

Myoseverin B is a microtubule assembly inhibitor that impedes tubulin polymerization (IC50 = 2 μM) and generally exhibits low cytotoxicity across most cell types. It is utilized in antitumor agent research.

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

Dynapyrazole A is a specific inhibitor of microtubule dynamin with IC50s of 2.3 and 2.6 μM for dynein 1 and dynein 2-dependent microtubule gliding, and it inhibits Hedgehog signaling with an IC50 of 1.9 μM.

Vinflunine ditartrate, a fluorinated microtubule inhibitor and member of the Vinca alkaloids family, exhibits anti-angiogenic, vascular-disrupting, and anti-metastatic properties. It presents a potential avenue for studying transitional cell carcinoma of the urothelial tract, non-small cell lung cancer, and breast carcinoma[1][2].

Sertaconazole is a broad-spectrum antifungal.

CK-869, an Actin-Related Protein 2 3 (ARP2 3) complex inhibitor with an IC50 of 7 μM, is a valuable tool for investigating the Arp2 3 complex.

KIF18A-IN-2 is an inhibitor of mitotic kinesin Kif18A with IC50 of 28 nM and can be used in studies about chromosomal instability-associated vulnerabilities.

Tubulin inhibitor 14 is a potent inhibitor of NQO2 (quinone oxidoreductase 2) with an IC50 of 1.0 μM, which also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. As a microtubule destabilizer, Tubulin inhibitor 14 has potential tumor-selective, anti-angiogenic, and vascular-destructive properties [1].