microtubule-destabilizing

Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective anticancer compound targeting microtubule proteins. It disrupts microtubule stability, inhibiting microtubule polymerization. This agent causes human tumor cells to arrest in the G0 G1 phase and induces apoptosis (Apoptosis) through activation of the Caspase cascade pathway. Additionally, it exhibits anti-inflammatory properties, inhibiting the production of TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 also suppresses tumor growth in xenograft mice.

Compound 12b (Microtubule Destabilizing Agent-1), a hydroxamic acid-based microtubule destabilizing agent (MDA), exhibits potent antitumor activity, favorable metabolic stability, and high bioavailability, making it a promising candidate for further investigation as an MDA [1].

Vincristine sulfate is an alkaloidal natural product that binds to microtubule proteins and inhibits the formation of microtubules, thereby inhibiting mitosis in tumor cells. Vincristine sulfate is used as a microtubule destabilizing agent in research studies for the treatment of hematologic neoplasms such as leukemias and lymphomas, as well as in studies related to sarcomas in children.

Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.

CHM-1 is an inducer of apoptosis, and displays potent antitumor ability in human hepatocellular carcinoma by activation of Cdc2 kinase activity. CHM-1 inhibits tubulin polymerization in vitro and in vivo.

Tubulysin B is an agent of potent microtubule destabilizing and highly cytotoxic peptide isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis.

Tubulysin family are originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis, and are potent microtubule destabilizing agents.

Podoverine A is a microtubule destabilizing natural product from the Podophyllum species.

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

Antiproliferative agent-23, a microtubule-destabilizing agent (MDA), disrupts the tubulin-microtubule system, leading to apoptosis through a mitochondrion-dependent pathway. This involves downregulation of Bcl-2 protein, upregulation of Bax and Cyt c proteins, and activation of the caspase cascade. Additionally, it induces reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549 CDDP cells (cisplatin-resistant cancer cell line) through the PERK ATF4 CHOP signaling pathway, demonstrating anti-tumor activity [1].

Taccabulin A, a new retro-dihydrochalcone, with microtubule-destabilizing activity has been identified from the roots and rhizomes of Tacca species.