Sinalização Citoesquelética

<p>Row174336 (compound 29) serves as an efficient inhibitor of the Hsp110-STAT3 interaction, exhibiting antiproliferative activity in the HPAEC cell line with an IC50 of 22.67 μM.</p>

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

<p>Tubulin polymerization-IN-75 (Compound 6) is an inhibitor of tubulin polymerization, with an IC50 value of 30 μM. It effectively suppresses the proliferation of cancer cells Huh7 and 293T, demonstrating IC50 values of 14.3 μM and 13.8 μM, respectively.</p>

<p>Wikstrol A: antifungal, anti-mitotic, anti-HIV agent with various IC50/MDC values (67.8-131 µM) and deforms P. oryzae mycelia.</p>

<p>EV206 is an effective inhibitor of Hsp70, exhibiting antiproliferative properties. This compound induces cell apoptosis (apoptosis) and enhances the protein expression of cleaved PARP and caspase-3. Additionally, EV206 demonstrates antitumor activity.</p>

<p>MT-134 is a SkMII -specific inhibitor and has excellent exposure in muscles.</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>Alfalone (compound 9ia) is an antimitotic agent. It induces cleavage arrest and initiates the formation of tubercular eggs.</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>Compound 13m, a difluoro derivative, activates Nrf2/HO-1, showing neuroprotective and antioxidant effects, useful in PD research.</p>

<p>L 734217 is an antagonist of the fibrinogen receptor.</p>

<p>POSH-IN-2 (MIDI) is a mitochondrial fission inhibitor and a DRP1 inhibitor that effectively prevents mitochondrial fragmentation caused by cellular stress and genetic mitochondrial damage. It covalently interacts with DRP1-C367 to target the interaction of DRP1 with multiple receptors.</p>

<p>GSK3335103 is a non-peptide, orally active inhibitor of αvβ6 integrin (pIC50=8), employed in the study of pulmonary fibrosis.</p>

<p>TACC3 inhibitor 2 (Compound 13b) is a TACC3 inhibitor with an IC50 of 200 nM. It induces mitotic arrest, apoptosis (Apoptosis), and DNA damage. TACC3 inhibitor 2 is applicable for research in the field of cancer.</p>

<p>Onalespib lactate is a second-generation, potent and selective HSP90 Inhibitor with antitumor activity.</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>Tubulin inhibitor 19 (9b), a potent indole chalcone, strongly blocks tubulin, valuable in cancer studies.</p>

<p>MKLP2-IN-1 (compound 12a) is an inhibitor of MKLP2 that demonstrates excellent oral bioactivity. In vitro, MKLP2-IN-1 inhibits the ATPase activity stimulated by recombinant MKLP2 microtubules and, in a mouse Calu-6 lung cancer model, it effectively suppresses tumor growth.</p>

<p>Fradafiban binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM. Fradafiban is a non-polypeptide platelet glycoprotein IIb/IIIa antagonist.</p>

<p>Compound IIc inhibits tubulin polymerization, arrests cell cycle at G2/M in HCT116 cells, IC50 12.7 μM, potential for cancer research.</p>

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

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

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

<p>FAK-IN-21 (compound 9) is a FAK inhibitor with an IC50 value of 37.52 nM. It inhibits cell growth and the phosphorylation of FAK, making it useful for research into diffuse gastric cancer.</p>

<p>Tubulin polymerization-IN-32: a cancer cell growth inhibitor used for research in cancers like lymphoma.</p>

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

<p>Terpendole E is an atypical L5 site inhibitor.</p>

<p>6-B345TTQ is an α4 integrin inhibitor that can impede the interaction between α4 and Leupaxin. This compound is applicable for studies focused on inflammation research.</p>

<p>Epothilone E, a derivative of epothilone, functions by inhibiting microtubule protein activity, thereby halting cell division and exhibiting anti-tumor</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>

<p>Lisavanbulin (BAL-101553) is a prodrug of Avanbulin (BAL 27862), a microtubule-targeting agent. It exhibits antitumor activity, particularly effective against tumors with high expression of end-binding protein 1.</p>

<p>TTBK1/2-IN-1 (compound 3) is a potent inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 816 nM and 384 nM, respectively.</p>

<p>Si306, an Src inhibitor, exhibits antitumor activity by reducing the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), thereby inhibiting the invasion of human glioblastoma (GBM).</p>

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

<p>Tubulin polymerization-IN-63 (compound 6) is an inhibitor of tubulin polymerization. It exhibits an IC50 value of 0.29 μM against MES-SA cells, making it suitable for use in cancer research.</p>

<p>Hsp90-IN-34 (compound HAM-1) is a chemical inhibitor that targets the Aha1-Hsp90 chaperone complex with high affinity (KDapp=23.5 µM). It modulates the ATPase activity of Hsp90 by affecting the interaction between Hsp90 and Aha1.</p>

<p>Icafolin-methyl is a plant-specific herbicide that acts as an inhibitor of tubulin polymerization. In plants, it metabolizes into the carboxylic acid icafolin, potentially inhibiting plant tubulin polymerization by binding to β-tubulin.</p>

<p>KU-32 is a novel and novobiocin-based Hsp90 inhibitor. It can protect against neuronal cell death.</p>

<p>AMG28 is an inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 805 nM and 988 nM, respectively. Additionally, AMG28 suppresses the phosphorylation of tau protein at the Ser422 site, with an IC50 of 1.85 μM.</p>

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

Sagopilone: synthetic epothilone, inhibits cell division and induces apoptosis, effective in MDR tumors, not P-gp substrate.

<p>Dioleyl phosphatidylserine is a phospholipid that can activate PKC-γ (Protein Kinase C-gamma) when the Ca2+ concentration is below 0.5 μM, specifically at a concentration of 100 μM.</p>

PKCTheta-IN-2 (compound 14) is a potent and selective inhibitor of PKCθ, with an IC50 value of 0.25 nM. It demonstrates good selectivity across a broad range of kinases, including the PKC subfamily (30 kinases). Additionally, PKCTheta-IN-2 effectively inhibits the production of IL-2 in mice, where it exhibits an IC50 of 682 nM.

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

<p>MonomethylauristatinE intermediate-17 is an intermediate compound used in the synthesis of MonomethylauristatinE. MonomethylauristatinE (MMAE) functions as a microtubule/tubulin inhibitor with anticancer properties. It is widely utilized as the cytotoxic component in antibody-drug conjugates (ADCs).</p>

<p>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.</p>

<p>Des-ethyl-carafiban (Compound 44) is an antagonist of the fibrinogen receptor, effectively inhibiting platelet aggregation induced by various agonists. It is useful for research in thrombotic diseases.</p>

<p>Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K/Akt/mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.</p>

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

<p>DDO-6691 is an inhibitor of heat shock protein 90 (HSP90). It exhibits antiproliferative effects against various tumor cells, with the highest sensitivity observed in HCT-116 colon cancer cells (IC50: 1.08 μM). DDO-6691 also demonstrates potent tumor growth inhibition in HCT-116 xenograft mouse models.</p>

<p>GSK3β-IN-2 (Compound S01) is an inhibitor of GSK3β with an IC50 of 0.35 nM. It activates the Wnt/β-catenin signaling pathway, promoting neurogenesis and neurite outgrowth. GSK3β-IN-2 reduces tau protein phosphorylation induced by Aβ at the Ser396 site, thereby decreasing neurofibrillary tangles. Furthermore, GSK3β-IN-2 improves Alzheimer's disease symptoms in a zebrafish model.</p>

<p>ETB is a potent inhibitor of Hsp60 chaperone activity. It can impede the chaperone function of both wild-type proteins and the C237A and C447A mutant proteins. ETB binds to Hsp60 at Cys442, and the C442A mutant demonstrates resistance to ETB inhibition.</p>

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

<p>GSD-11: Potent, selective anti-austerity agent; blocks Akt/mTOR pathway, hinders PANC-1 cell migration &amp; colony growth. Promising for pancreatic cancer study.</p>

<p>AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).</p>

<p>PROTACα-synuclein degrader 6 (compound T3) is a PROTAC degrader of α-synuclein and tau, with an EC50 of 1.57 μM and 4.09 μM, respectively. This compound plays a significant role in neurodegenerative disease (ND) research.</p>

<p>G-9791 is an effective and selective inhibitor of group-I PAK.</p>

<p>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.</p>

<p>HG-7-86-01 is a selective type II tyrosine kinase inhibitor with antiproliferative activity against mutant T315I- Bcr-Abl for chronic myeloid leukemia (CML).</p>

<p>KY-02327 acetate inhibits Dvl-CXXC5, stabilizes Wnt/β-catenin signaling, and enhances osteoblast differentiation.</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>SF0166: potent αvβ3 antagonist, IC50: 0.6 nM. Blocks cell adhesion, IC50: 7.6 pM-76 nM. Reduces neovascularization in mice.</p>

<p>KUNG65 acts as a selective Grp94 inhibitor, demonstrating a target dissociation constant (K_d) of 540 nM. It exhibits a minimum selectivity of 73-fold compared to other Hsp90 isoforms.</p>

<p>RMS-07, a covalent MPS1/TTK inhibitor, has an IC50 of 13.1 nM, targeting a kinase hinge cysteine.</p>

<p>Zalunfiban (RUC-4) is a potent αIIbβ3 platelet antagonist, IC50 45 nM, used in myocardial infarction research.</p>

<p>β-Catenin modulator-8 (Compound Ⅸa) is a specific β-catenin modulator for use in cancer research.</p>

<p>Tasidotin hydrochloride, a dolastatin 15 analog, inhibits microtubule assembly and dynamics.</p>

<p>α5β1 integrin agonist-1 is an α5β1 integrin agonist that selectively delivers 5-FU to tumour cells and induces tumour cell death.</p>

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

<p>NRX-103094 boosts β-catenin binding to SCFβ-TrCP ligase with EC50 62 nM and Kd 0.6 nM.</p>

<p>NRX-252114 promotes mutant β-catenin degradation, binding it to E3 ligase SCFβ-TrCP (EC50: 6.5 nM; Kd: 0.4 nM).</p>

<p>AKT Kinase Inhibitor is an Akt inhibitor with antitumor activity that selectively inhibits cell proliferation in a dose-dependent manner.Cost-effective and quality-assured.</p>

<p>Ombrabulin is a derivative of CA-4 phosphate. It is known to show antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.</p>

<p>24-Methylenecycloartanyl ferulate, a compound belonging to the γ-oryzanol family, demonstrates the ability to enhance parvin-beta expression within human breast cancer cells. Furthermore, it exhibits potential as an ATP-competitive Akt1 inhibitor, with an EC 50 value of 33.3 μM.</p>

<p>20-HETE is a CYP450 product, vasoconstrictor, modulates K+ channels, affects NADPH, ROS, NF-κB, NO synthase, and cell apoptosis/proliferation.</p>

<p>ZW4864 is a selective inhibitor of the β-catenin/B-Cell Lymphoma 9 protein (β-catenin/BCL9 PPI) interaction, demonstrating oral activity. It inhibits β-catenin/BCL9 PPI with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM.</p>

<p>Tau tracer 2 (Pl-2620) is a specific imaging agent designed to detect and visualize Tau protein aggregates, primarily used for diagnosing neurodegenerative diseases [1].</p>

<p>Cercosporin, produced by the plant pathogen Cercospora kikuchii and the elsinochromes, is a potent photosensitizer with a short activation wavelength. Cercosporin contains perylene quinone structural features essential for PKC activity (IC50: 0.6-1.3 μM).</p>

<p>Sevasemten is an allosteric inhibitor that targets skeletal muscle myosin. It displays selectivity in its inhibition, demonstrated by IC50 values of ≤10 μM for skeletal muscle myosin and &gt;100 μM for cardiac myosin, respectively.</p>

<p>PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.</p>

<p>Cevipabulin (TTI-237) fumarate is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).</p>

<p>CMX-2043 is a drug potentially to block oxidative damage and activate cell survival pathways.</p>

<p>BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor featuring a trimethoxy group [1].</p>