tubulin-inhibitory

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.

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.

Valecobulin hydrochloride (CKD-516 hydrochloride) is the valine prodrug and vasoblocker of S516. Valecobulin hydrochloride (CKD-516 hydrochloride) has a potent inhibitory effect on β-tubulin polymerization and has significant anti-tumor activity against solid tumors in mice and humans.

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM.

GGFG-PAB-MMAE (Comp 58054-1) is a drug-linker conjugate for ADC that comprises an ADC linker (GGFG-PAB) and the potent tubulin polymerization inhibitor, MMAE. This formulation combines the targeted delivery mechanism inherent in ADC technology with the effective inhibitory action of MMAE against tubulin polymerization.

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.

Dolastatin 10 trifluoroacetate is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have an activity to inhibit tubulin polymerization (IC50: 1.2 μM). Besides that, it

PARP1-IN-6, a dual-function inhibitor, targets both tubulin and PARP-1, demonstrating inhibitory concentration (IC50) values of 0.94 μM for tubulin and 0.48 μM for PARP-1.

Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and

TTBK1-IN-1 (compound 31) is a potent and selective tau microtubule protein kinase 1 (TTBK1) inhibitor (IC50=315 nM) with central nervous system (CNS) penetration that inhibits tau phosphorylation at the disease-associated Ser 422 epitope, and can be used to study Alzheimer's disease.

Tubulin inhibitor 12 (Hit 9) is a recently developed compound with potent tubulin inhibitory effects (IC50 = 25.3 μM) and significant anti-tumor and anti-proliferative activities, making it a promising candidate for cancer treatment [1].

HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1]

Tubulin inhibitor 19 (compound 9b) is a potent indole chalcone compound exhibiting strong tubulin inhibitory activity, making it valuable for cancer research [1].

EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR tyrosine kinase (EGFR-TK) inhibitor with an IC50 of 0.054 μM. It also inhibits VEGFR-2, CK2α, topoisomerase IIβ, and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13, and 3.61 μM, respectively. The compound promotes cell cycle arrest at the G2 M and pre-G1 phases and induces apoptosis in cancer cells [1].

Antitumor Agent-71 is an antitumor compound that exhibits an inhibitory effect on tubulin aggregation. antitumor Agent-71 possesses an anti-proliferative effect with IC50 values ranging from 3.98-15.70 μM against tumor cell lines.

HDAC-IN-9 is a potent and selective dual inhibitor of tubulin and HDAC, exhibiting inhibitory effects on the invasion and migration of A549 cells, as well as potent anti-tumor and anti-angiogenic activities both in vitro and in vivo.

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4 SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

Tubulin Inhibitor 31 is a potent compound with an inhibitory concentration (IC 50) of 4 µM, demonstrating significant anti-proliferative activity and the ability to inhibit HUVEC migration.

Tubulin MMP-IN-2, a dual inhibitor of tubulin and matrix metalloproteinases (MMPs), effectively inhibits tubulin polymerization and induces cell apoptosis. It demonstrates inhibitory activities against MMP-2, MMP-3, and MMP-9, with IC50 values of 24.95 μM, 31.60 μM, and 22.37 μM, respectively. This compound is utilized in cancer research.

HI5, a potent inhibitor of tubulin and indoleamine 2,3-dioxygenase (IDO), exhibits an inhibitory concentration (IC50) of 70 nM in HeLa cells. It suppresses IDO expression, reduces kynurenine production, and enhances T cell activation and proliferation. Additionally, HI5 impedes tubulin polymerization and cell migration, induces G2 M phase arrest, and leads to apoptosis through the mitochondrial-dependent apoptosis pathway while generating reactive oxidative stress in HeLa cells, making it a valuable compound for anticancer research.

3,4',5-Trismethoxybenzophenone (compound 16a) is an effective inhibitor of tubulin assembly, demonstrating a half-maximal inhibitory concentration (IC 50) of 2.6 µM [1].

ABT-751 (E7010) hydrochloride is a novel sulfonyl anti-mitotic compound and a tubulin binder with high oral bioavailability. This agent binds to the colchicine site on β-tubulin, inhibiting the polymerization of tubulin which results in cell cycle arrest at the G2 M phase and induces apoptosis, effectively preventing cell division. Additionally, ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT MTOR signaling pathway. It exhibits significant inhibitory effects against various types of cancer cells, including lung, stomach, colon, and breast cancer.