destabilizing

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.

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.

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.

Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of Y cells and to exhibit a potent anticancer activity in vivo.

Anticanceragent 270 (Compound 8e) is a microtubule protein inhibitor with an IC50 of 1.02 μM against MCF-7 breast cancer cells. It exerts significant antiproliferative activity on breast cancer cells through a dual mechanism of inducing apoptosis and destabilizing microtubules. Anticanceragent 270 is useful for cancer research.

I3IN-002 is a small molecule inhibitor targeting the RNA-binding protein IGF2BP3, with an IC50 value of approximately 2 μM in SEM cells. It disrupts the interaction with m6A-modified mRNA, destabilizing target genes (such as CDK6, MYC, and BCL2), thereby inhibiting the growth of leukemia cells, inducing cell cycle arrest, and promoting apoptosis. I3IN-002 shows potential for research in B-cell acute lymphoblastic leukemia.

VNT-101 is an orally active inhibitor of influenza A virus (IAV). It disrupts NP-NP protein interactions, preventing NP oligomerization and destabilizing the viral ribonucleoprotein (RNP) complex, showing potent antiviral activity against multiple influenza A virus subtypes. In cell-based cytopathic effect (CPE) assays, VNT-101 has an EC50 value of 4-5 nM, while it measures 4-8 nM in neuraminidase (NA) assays and 21-45 nM in ribonucleoprotein (RNP) assays. Demonstrating strong in vivo antiviral efficacy, VNT-101 protects against lethal H1N1 virus infection in mice. VNT-101 is applicable to influenza A virus infection research.

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.

Shield-2 is a potent FKBP-derived destabilizing domain stabilizing ligand.

CMP3a is a NEK2 kinase inhibitor. CMP3a efficiently attenuated GBM growth in a mouse model and exhibited a synergistic effect with radiotherapy. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase E

IMC-76 is a BCL2 i-motif-interactive compound that can act by destabilizing or unfolding the i-motif.

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

Siramesine (Lu 28-179)(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.lysosome-destabilizing agent siramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost

DAP-81 is a diaminopyrimidine derivative that targets PLKs, destabilizing kinetochore microtubules. Other spindle tubules are stabilized, resulting in monopolar mitotic spindles. In vitro, DAP-81 inhibits Plk1 at an IC50 of 0.9 nM. DAP-81 is currently in ongoing preclinical evaluations.

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......

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].

Thanatin acetate is a cationic peptide with antimicrobial activity, inhibiting the growth of bacteria and fungi by targeting the LptC-LptA interaction and destabilizing the LptA complex involved in lipopolysaccharide transport.

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

Onc112 is a proline-rich antimicrobial peptide that exhibits potent activity against Gram-negative bacteria. It functions by inhibiting translation through blocking and destabilizing the initiation complex.