Cytoskeletal Signaling

<p>KAA, an anticancer compound, inhibits centrosome clustering and targets HSET+ yeast and cancer cells.</p>

<p>Tubulin-IN-33, an oxazoloisoindole, hinders microtubule assembly; effective against NCI cancer cells.</p>

<p>TPI 287: synthetic taxane; may halt cancer by stabilizing microtubules, blocking cell division, inducing apoptosis.</p>

<p>Compound 24: Potent Nrf2/HO-1 activator with neuroprotective, antioxidant properties; useful in PD research.</p>

<p>Tubulin-IN-35 inhibits oxazolylisoindole microtubule formation, targeting VL51 marginal zone lymphoma.</p>

<p>Onalespib lactate is a second-generation, potent and selective HSP90 Inhibitor with antitumor activity.</p>

<p>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.</p>

<p>Tubulin inhibitor 49 (Compound 18) is an inhibitor of tubulin polymerization with an IC50 of 48 μM. It disrupts the microtubule network of cells, causing cell cycle arrest in the G2 phase, and exhibits cytotoxicity with an IC50 of 8.8 μM in HeLa cells.</p>

<p>Quinagolide hydrochloride is a selective agonist of dopamine D2 receptor.</p>

<p>XD23 is a potent osteosarcoma inhibitor that functions by downregulating DKK1 and activating the WNT/β-catenin signaling pathway.</p>

<p>HSP90-IN-9: potent HSP90 inhibitor, dose-dependent fungicide, impedes biofilm/morphology with FLC, reverses FLC resistance.</p>

<p>AChE/GSK-3β-IN-1 is a potent dual AChE/GSK-3β inhibitor that crosses the blood-brain barrier and acts on hAChE (IC50: 1.2 nM), hBChE (IC50: 149.8 nM) and hGSK-</p>

<p>SPA0355 is a thiourea derivative with antioxidant and anti-inflammatory properties. It inhibits RANKL (receptor activator of nuclear factor κB ligand)-induced osteoclastogenesis in primary bone marrow-derived macrophages and suppresses the activation of MAPKs, Akt, and NF-κB pathways. Furthermore, SPA0355 enhances osteoblast differentiation by increasing alkaline phosphatase activity and mineralized nodule formation. It protects ovariectomized mice from bone loss by stimulating osteoblast differentiation and inhibiting osteoclast resorption, making it a potential candidate for studying postmenopausal osteoporosis.</p>

<p>SF0166: potent αvβ3 antagonist, IC50: 0.6 nM. Blocks cell adhesion, IC50: 7.6 pM-76 nM. Reduces neovascularization in mice.</p>

<p>HSN748 is an analog of ponatinib and acts as a multi-kinase inhibitor. It exhibits inhibitory activity against kinases such as FLT3, ABL1, RET, PDGFRα/β, MNK1, and MNK2. HSN748 can suppress the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines, making it a useful compound in leukemia research.</p>

<p>Ethaboxam is a β-tubulin inhibitor and antifungal agent used against oomycete pathogens.</p>

<p>AKT-IN-26 (Compound 453) is an AKT inhibitor that binds to the Pleckstrin Homology (PH) domain of AKT. It is useful for research related to cell proliferation and cancer involving the AKT pathway.</p>

<p>Hsp90-IN-38 (compound 20m) is an inhibitor of HSP90 (heat shock protein). It demonstrates a strong binding affinity to HSP90 with a Kd of 87 nM. The compound inhibits ATPase activity with an IC50 of 0.13 μM. Hsp90-IN-38 also shows inhibitory effects on HCT116, MCF-7, SKBr3, K562, and A549 cells with IC50 values of 0.187, 0.072, 0.105, 0.403, and 0.031 μM, respectively.</p>

<p>NAP1051, a biomimetic analog of Lipoxin A4, serves an anti-tumor role by targeting the inflammatory tumor microenvironment. It inhibits the chemotaxis of neutrophils to fMLP and stimulates macrophage efferocytosis by activating AKT. NAP1051 is utilized in research on colorectal cancer.</p>