Tubulin inhibitor 7

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 inhibitor 24 is a potent compound that inhibits tubulin polymerization.

CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. It also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

Sertaconazole nitrate (FI-7045), a topical broad-spectrum antifungal, is developed to supply an additional agent for the treatment of superficial cutaneous and mucosal infections.

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.

Antiproliferative agent-59 (Compound 14u) acts as an inhibitor of tubulin polymerization. Demonstrating anticancer activity in Huh7, SGC-7901, and MCF-7 cell lines, this compound achieves IC50 values of 0.03, 0.18, and 0.13 μM, respectively. Additionally, it arrests the cell cycle at the G2 M phase and induces apoptosis in Huh7 cells. In a xenograft mouse model utilizing Huh7 cells, Antiproliferative agent-59 exhibits antitumor effects against hepatocellular carcinoma without significant toxicity.

Antiproliferative agent-64 (Compound 76) functions as an inhibitor of the eukaryotic translation initiation factor 4E (eIF4E) and disrupts the secondary structure of mRNA, thereby hindering protein translation. It inhibits the 5' untranslated region (5'UTR) of c-Myc with an EC50 of 1.2 nM and the 5'UTR of tubulin with an EC50 of 40 nM. Additionally, Antiproliferative agent-64 suppresses the proliferation of MDA-MB-231 cells with an EC50 of 7 nM.

HDAC-IN-82 (Compound 18b) is a histone deacetylase (HDAC) inhibitor that demonstrates selective antimalarial and anticancer activities. It shows significant antiproliferative and caspase3 7 activity in tumor cells. Additionally, HDAC-IN-82 induces hyperacetylation of histone H3 and α-tubulin.

MT-7 is a tubulin polymerization inhibitor.

1. 7-epi-Taxol (7-Epitaxol) is the major derivative of taxol found in cells and that its presence does not alter, in a major way, the overall biological activity of taxol.

Thiocolchicine is an effective inhibitor of tubulin polymerization with an IC50 of 2.5 µM and a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

Sertaconazole is a broad-spectrum antifungal.

10-Deacetyl-7-xylosyl paclitaxel (7-Xylosyl-10-deacetyltaxol) is a Paclitaxel derivative with improved pharmacological features and higher water solubility,used in Chinese clinics to treat cancer.

Antitumor agent-68 is a potent tubulin inhibitor exhibiting significant antitumor activity, with IC 50 values of 3.6 μM for HeLa and 3.8 μM for MCF-7 cells. It also demonstrates good scavenging activity of ROS and DPPH radicals in a dose-dependent manner [1].

Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor that disrupts tubulin assembly by binding at the colchicine site (IC50 = 1.2 μM), and exhibits antiproliferative effects on MCF-7 cells with an IC50 value of 7.5 μM. [1].

Tubulin polymerization-IN-24 (compound HMBA) is a potent inhibitor of tubulin polymerization, increasing GTP hydrolysis rate and inhibiting microtubule assembly. It induces apoptosis and cell cycle arrest in the G2 M phase, and inhibits the proliferation of MCF-7 cells [1].

Tubulin Inhibitor 28 (compound 2g), with an IC50 value of 1.2 μM, is a potent inhibitor of tubulin that exhibits significant anti-proliferative activity against MCF-7 cells [1].

Tubulin aggregation-IN-7 is a potent tubulin aggregation inhibitor that has shown research potential for cancer diseases.

ER degrader 7 (Compound 35t) is a selective degrader of both ERα and ERβ and functions as a tubulin polymerization inhibitor. It inhibits cell viability with IC50 values of 0.06 μM for MCF-7, 2.56 μM for T47D, 15.84 μM for MCF-10A, 1.59 μM for LCC2, 1.67 μM for T47D D538G, and 1.37 μM for T47D Y537S cells. Additionally, ER degrader 7 demonstrates efficacy in suppressing breast cancer tumor growth [1].

Tubulin polymerization-IN-46 (compound 9q) is a microtubule tubulin inhibitor that obstructs tubulin polymerization, triggers apoptosis, and arrests MCF-7 breast cancer cells in the G2 M phase, demonstrating potent anti-proliferative activity with an IC50 of 10 nM [1].

LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2 M arrest.