Cytoskeletal Signaling

AKT-IN-11 is one of the most potent antibacterial agents against human hepatocellular carcinoma Bel-7402 cell line (IC50: 1.15 μM).

NRX-2663 boosts β-catenin binding to E3 ligase SCFβ-TrCP (Kd: 54.8 nM, EC50: 22.9 nM).

<p>Tubulin inhibitor 15 is a potent tubulin inhibitor with antiproliferative activity. Tubulin inhibitor 15 exhibits cytotoxicity in HepG2 cells [1].</p>

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

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

<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>

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

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-

JC168 is a phenyl analog of peloruside and functions as a microtubule inhibitor with antiproliferative and anticancer properties. It enhances tubulin polymerization, thereby disrupting microtubule dynamics, making it a useful agent in the study of microtubule-associated diseases.

APN/AKT-IN-1, a dual APN (IC50=0.21μM) & AKT (IC50=0.27μM) inhibitor, hinders GSK3β phosphorylation.

AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).

Myoseverin B is a microtubule assembly inhibitor that impedes tubulin polymerization (IC50 = 2 μM) and generally exhibits low cytotoxicity across most cell types. It is utilized in antitumor agent research.

KY-02327 acetate inhibits Dvl-CXXC5, stabilizes Wnt/β-catenin signaling, and enhances osteoblast differentiation.

HSP90-IN-11: potent HSP90 inhibitor, akin to AUY-922; hinders CRC/NSCLC cell proliferation; degrades EGFR, Akt proteins.

Antitubulin agents-1 disrupts microtubules, ups α-tubulin acetylation, and has anticancer properties.

<p>Alfalone (compound 9ia) is an antimitotic agent. It induces cleavage arrest and initiates the formation of tubercular eggs.</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>

Tau ligand-1 (Compound 75) is a ligand of aggregated tau protein that can penetrate the blood-brain barrier. In tissues affected by Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 shows high affinity for aggregated tau protein, with equilibrium dissociation constants (KD) ranging from 1 to 3.8 nM. It holds potential as a positron emission tomography (PET) tracer for imaging studies of tau-related diseases within the central nervous system.

<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>

AKT-IN-10, a potent AKT inhibitor, has potential for breast and prostate cancer research, impacting cell growth and survival pathways.