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.

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.

Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor that binds to the colchicine site on tubulin, causing G2/M cell cycle arrest and inducing reactive oxygen species (ROS) production. It demonstrates significant inhibitory activity against P-glycoprotein (P-gp) overexpressing cell lines MCF7/ADR and KBV200, with resistance indices (DRI) of 0.83 and 0.58, respectively. In an MCF-7 xenograft model, Antitumor agent-200 (at 25 mg/kg, administered intraperitoneally) achieves a 57.2% tumor growth inhibition rate. This compound is applicable for research in the field of cancer therapy.

Taltobulinintermediate-7 is an intermediate in the synthesis of Taltobulin. Taltobulin is a commonly used toxin component in ADC preparation (ADC Cytotoxin) and serves as a potent inhibitor of microtubule/tubulin. It disrupts microtubule polymerization, induces mitotic arrest, and triggers apoptosis [apoptosis].

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 inhibitor 9 (compound 7) is a microtubule (Tubulin) inhibitor with anticancer activity, demonstrated by an IC50 of 0.9 nM in MDA-MB 231 cells.

Tubulin-IN-53 is a potent inhibitor of microtubulin (Tubulin) with an IC50 of 6.06 μM. By targeting the colchicine binding site on tubulin, Tubulin-IN-53 hinders tubulin polymerization, disrupting the microtubule network. It induces cell cycle arrest at the G2/M phase and apoptosis (apoptosis) in MCF-7 cells, while inhibiting cell migration. This compound also leads to a reduction in mitochondrial membrane potential and an increase in reactive oxygen species (ROS) accumulation. Additionally, Tubulin-IN-53 disrupts angiogenesis in human umbilical vein endothelial cells and is applicable in research on cancers such as breast and lung cancer.

Ferroptosisinducer-9 is an agent that induces ferroptosis and acts as a microtubule polymerization inhibitor at the colchicine binding site. It inhibits MCF-7 cell growth with an IC50 of 14 nM and reduces [3H]colchicine binding. The compound decreases GPX4 and FTH expression while increasing COX2 and ACSL4 levels; it also lowers GSH, NADP+, and NADPH, and raises LPO, MDA, and Fe(II) concentrations, alongside reducing SOD levels. Ferroptosisinducer-9 demonstrates significant antitumor efficacy in HCT116 CRC xenograft models and is applicable in the study of triple-negative breast cancer (TNBC) and colorectal cancer (CRC).

HDAC6-IN-67 is a selective HDAC6 inhibitor with an IC50 of 17.15 nM, demonstrating 19-fold selectivity over HDAC1. It selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by cleaving caspase9, 8, 3 and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. It effectively acetylates α-tubulin in MCF-7/ADR cells without affecting histone H3 acetylation. HDAC6-IN-67 is applicable in breast cancer research.

Tubulin polymerization-IN-85 (Compound C21) is a microtubule polymerization inhibitor with an IC50 value of 1.59 μM, targeting the colchicine binding site. It exhibits antiproliferative activity against HeLa, HepG2, MCF-7, and A549 cells with IC50 values of 0.08, 0.21, 0.27, and 0.32 μM, respectively, while demonstrating low toxicity to normal renal epithelial 293T cells (IC50 value of 187 μM). Tubulin polymerization-IN-85 induces G2/M phase arrest and triggers apoptosis in cancer cells. It downregulates the expression of Bcl-2, Bcl-xl, Mcl-1, Cyclin B1, cdc25, and cdc2 proteins, and upregulates P53, P21, Bad, and Bax levels. This compound is applicable in cancer research, such as cervical cancer studies.

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].