γ-tubulin

Ciliobrevin D is a AAA+ ATPase motor cytoplasmic dynein inhibitor. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation and it also inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.

Tubulin inhibitor 24 is a potent compound that inhibits tubulin polymerization.

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

Tubulin inhibitor 1 is an inhibitor of tubulin, inhibits tubulin polymerization, with potent anti-tumor activity, induces cellular apoptosis causes and cellular mitotic arrest in the G2/M phase.

Tubulin Inhibitor 11 is a potent, orally active agent that inhibits tubulin by targeting the Colchicine binding site. It impedes tubulin polymerization, leading to mitotic blockade and apoptosis.

Tubulin inhibitor 35 (Tubulin IN 35) is a potent dual inhibitor of topoisomerase I and microtubule protein polymerization with antitumor activity, inhibits migration and invasion of MGC-803 and RKO cell lines, interrupts the cell cycle and induces apoptosis.

Tubulin inhibitor 32 is an orally active novel microtubule inhibitor with antiproliferative and antitumor activity, inhibits microtubule polymerization, induces apoptosis and cell cycle arrest in G2/M phase.

Tubulin polymerization-IN-47 is a tubulin polymerization inhibitor and mitotic inhibitor with antitumor activity and inhibitory effects on neuroblastoma cancer cell proliferation, with IC50s of 7 and 12 nM for Chp-134 and Kelly cell lines, respectively. Tubulin polymerization-IN-47 is a candidate compound for the treatment of hepatocellular carcinoma, colon cancer, lung cancer and breast cancer.

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 inhibitor 7 is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines (tubulin polymerization (IC50: 0.52 μM), K562 cell growth (IC50: 11 nM)).

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 inhibitor 48 (compound 16) is an anticancer agent targeting microtubules. It exhibits IC50 values of 0.1 μM and 0.07 μM against LN-229 and Capan-1 cells, respectively.

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/MMP-IN-3 (Compound 15j) is a dual inhibitor of tubulin polymerization and MMP, effectively inhibiting MMP-2 and MMP-9 with IC50 values of 21.13 μM and 19.24 μM, respectively. It disrupts the NF-κB signaling pathway, leading to mitochondrial dysfunction and mitochondrial-dependent apoptosis. Tubulin/MMP-IN-3 shows antiproliferative activity in various cancer cells by causing cell cycle arrest at the G2/M phase and demonstrates antitumor effects in mouse models.

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.

TopoII/tubulin-IN-1 (Compound 1B8) is an inhibitor of TopoII/tubulin. It effectively suppresses the proliferation of tumor cells and reduces ROS levels, while inducing apoptosis and cell cycle arrest, without showing significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 exhibits antitumor activity.

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.

Tubulin-IN-52 is a potent, selective tubulin polymerization inhibitor with an IC₅₀ of 2.9 μM. Tubulin-IN-52 induces apoptosis in tumor cells by triggering a caspase cascade via the mitochondrial apoptosis pathway. Tubulin-IN-52 significantly inhibits tumor growth without significant toxicity. Tubulin-IN-52 can be used in cancer-related research.