β-tubulin polymerization

Tubulin polymerization-IN-55 is a potent Tubulin Polymerization inhibitor with potential anti-angiogenic and anti-tumor activity, demonstrating anti-proliferative effects against A549, K562, HepG2, MDA-MB-231, and HFL-1.

Tubulin polymerization-IN-43 is an inhibitor of tubulin polymerisation.Tubulin polymerization-IN-43 has multiple effects, disrupting the cellular microtubule network by targeting the colchicine locus and promoting cell cycle arrest and apoptosis in leukaemia cells. Tubulin polymerisation-IN-43 has multiple effects, promoting leukaemia cell cycle arrest in G2/M phase and apoptosis by targeting Colchicine sites to disrupt the cellular microtubule network.

Tubulin polymerization-IN-62 (Compound 14b) is a microtubule polymerization inhibitor (IC50 of 7.5 μM) that also functions as a degradation agent for α-/β-tubulin. This compound suppresses the proliferation of cancer cells MCF-7, A549, and HCT-116 with IC50 values of 32, 60, and 29 nM, respectively. It induces G2/M phase cell cycle arrest and inhibits the migration of MCF-7 cells. In a 4T1 syngeneic mouse model, Tubulin polymerization-IN-62 demonstrates antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27%.

Tubulin polymerization-IN-83 (Compound A23) is a flavonol derivative with antifungal activity against various plant pathogenic fungi. It has an EC50 of 0.338 μg/mL against Botrytis cinerea. The compound works by targeting β-tubulin, disrupting hyphal morphology, and affecting cell membrane permeability, while posing low ecological risk.

Tubulin Polymerization-IN-2 is a powerful anticancer agent that targets β-tubulin, exhibiting an IC 50 of 0.92 μM. It demonstrates promising efficacy against a range of cancer cell lines including leukemia, non-small cell lung, renal, prostate, and breast cancers [1].

Tubulin polymerization-IN-53 (compound 4b) inhibits β-tubulin polymerization, arrests the cell cycle at the G2/M stage, and demonstrates antiproliferative efficacy against the MDA-MB-231 cell line, with an IC50 value of 3.24 μM [1].

Tubulin polymerization-IN-68 (compound 32) serves as a tubulin inhibitor, disrupting cellular microtubule networks by hindering tubulin polymerization. It also upregulates PARP-1 and caspase-3 expression, thereby inducing apoptosis and exhibiting anticancer properties. Notably, Tubulin polymerization-IN-68 effectively suppresses HepG2 cells with an IC50 of 93 nM and markedly reduces the growth of HepG2 xenograft tumors in nude mice through oral administration.

Tubulin polymerization-IN-69 (compound 6c) exhibits significant inhibition of microtubule assembly in vitro, with an inhibition rate of 78.3% and an IC50 value of 6.53 μM. It rapidly induces apoptosis and G2/M phase cell cycle arrest in MCF-7 cells.

Tubulin polymerization-IN-70 (compound Q19) is an effective inhibitor of tubulin polymerization. This compound exerts antiproliferative properties by targeting the colchicine binding site on tubulin, thereby inhibiting its polymerization. Tubulin polymerization-IN-70 also induces apoptosis and cell cycle arrest at the G2/M phase. Additionally, it triggers a decrease in mitochondrial membrane potential and elevates levels of reactive oxygen species (ROS). Moreover, Tubulin polymerization-IN-70 possesses anti-angiogenic and anticancer activities.

Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a microtubule polymerization inhibitor prodrug mediated by Pd. Developed from colchicine-binding site inhibitors (CBSIs), it aims to reduce toxicity and enhance targeted release. Compared to the parent compound, its cytotoxicity is decreased by 68.3 times, but can be in situ restored in the presence of Pd resin. Mechanistic studies show it retains the same antitumor activity as CBSIs. In vivo tests demonstrate that, once activated by Pd resin, it significantly suppresses tumor growth (63.2% inhibition rate). Tubulin Polymerization-IN-1 prodrug is a promising candidate for cancer research.

Tubulin polymerization-IN-71 (Compound 4k) is an inhibitor of tubulin polymerization with an IC50 of 3.06 μM. It suppresses the proliferation of cancer cells MG-63 and U2OS, with an IC50 ranging from 0.08 to 0.14 μM. Additionally, Tubulin polymerization-IN-71 induces cell cycle arrest at the G2/M phase and triggers apoptosis in MG-63 cells.

Tubulinpolymerization IN-59 ((R) -9k) is an effective inhibitor of CBSI (colchicine binding site).

Tubulin polymerization-IN-73 (Compound 37) is an inhibitor of microtubule polymerization with an IC50 of 1.8 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in A549 cells. The compound inhibits the proliferation of both A549 WT and A549/T resistant cells with IC50 values of 0.023 μM and 0.057 μM, respectively. Additionally, Tubulin polymerization-IN-73 demonstrates antitumor activity in mouse models.

Tubulin polymerization-IN-75 (Compound 6) is an inhibitor of tubulin polymerization, with an IC50 value of 30 μM. It effectively suppresses the proliferation of cancer cells Huh7 and 293T, demonstrating IC50 values of 14.3 μM and 13.8 μM, respectively.

Tubulin polymerization-IN-74 (compound 11) is an inhibitor of tubulin polymerization, with an IC50 value of 15 μM. It is applicable to cancer research.

Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.

Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active inhibitor of tubulin polymerization. It acts at the colchicine binding site to inhibit tubulin polymerization with an IC50 value of 2.505 μM, effectively disrupting the intracellular microtubule network and interfering with mitosis. Tubulin polymerization-IN-76 shows significant inhibitory effects on MGC-803 and HGC-27 cells, with IC50 values of 1.61 and 1.82 nM, respectively. It effectively suppresses colony formation and cell migration activities in these cell lines, inducing G2/M phase cell cycle arrest and apoptosis (Apoptosis). Furthermore, Tubulin polymerization-IN-76 exhibits broad-spectrum antiproliferative activity.

Tubulin polymerization-IN-77 (Compound 15c) is a microtubule polymerization inhibitor that exhibits anti-glioblastoma activity by hindering microtubule polymerization. It demonstrates significant blood-brain barrier permeability, effectively induces G2/M phase arrest in GBM cells, and triggers apoptosis, while also markedly inhibiting tumor cell migration.

α-Tubulin polymerization-IN-1 (Compound 8l) functions as an inhibitor of α-tubulin polymerization. This compound modulates the NRF2/KEAP-1 signaling pathway and induces ROS production in PC-3 cells, leading to apoptosis. It inhibits the proliferation of PC-3 cells with a GI50 of 0.17 µM, causing cell cycle arrest in the G2/M phase. Additionally, α-Tubulin polymerization-IN-1 demonstrates antitumor activity in mouse models.

Tubulin polymerization-IN-78 (compound 10a) is an inhibitor of tubulin polymerization, with an IC50 value of 2.69 μM. It exhibits antiproliferative activity.

Tubulin polymerization-IN-58 (Compound K18) functions as a tubulin polymerization inhibitor with an IC50 of 0.446 μM. It also induces the degradation of the oncogenic protein YAP via the UPS pathway, making it a valuable tool for cancer research.

Tubulin polymerization/V-ATPase-IN-1 (compound F10) is an inhibitor of tubulin polymerization and V-ATPase. It exhibits potent antiproliferative activity against four types of human cancer cells by inhibiting both tubulin and V-ATPase. The compound also induces apoptosis and immunogenic cell death while suppressing tumor growth in the RM-1 allograft model with enhanced T lymphocyte infiltration.

Tubulin polymerization-IN-64 (Compound 8a) is a microtubule polymerization inhibitor that functions by occupying the colchicine binding site on tubulin, with an IC50 of 6.9 μM. This compound suppresses the proliferation of cancer cell lines A549, HeLa, HCT116, and HT-29, with IC50 values of 2.42, 10.33, 6.28, and 5.33 μM, respectively. Tubulin polymerization-IN-64 induces cell cycle arrest at the G2/M phase and triggers apoptosis in A549 cells.

Tubulin polymerization-IN-66 (Compound 13) inhibits colony formation and tubulin polymerization while also inducing apoptosis. It reduces cell viability in A549, A2780, SKOV3, and HCC827 cells, with IC50 values of 0.84, 0.38, 0.31, and 0.34 nM, respectively. Additionally, Tubulin polymerization-IN-66 is effective against the Paclitaxel-resistant A2780/T cancer cell line as well as its parent cell line, A2780.