cytoskeletal

GFB-8438 是有效的TRPC5选择性抑制剂，对 hTRPC5 和 hTRPC4 的IC50分别为 0.18 和 0.29 μM。它对 TRPC6、其他 TRP 家族成员、NaV1.5 具有良好的选择性，对 hERG 通道的活性也有限。它对小鼠足细胞的保护作用。

ROCK2-IN-10是一种有效的ROCK抑制剂，广泛应用于细胞迁移、侵袭、分化、增殖、免疫反应、抗药性、细胞骨架动态等研究领域。

PAIB-SOs-12 是一种抗有有丝分裂化合物,在低浓度下显示出抗增殖活性，诱导 MCF7 细胞细胞骨架损伤。

Endosidin 7(内苷 7)是一种特异性的胼胝质（Callose）合成酶抑制剂，在植物细胞质分裂期间组织胼胝质沉积，不影响间期或细胞骨架组织期间的内膜运输，阻止细胞后期分裂。

Erianin 能抑制吲哚胺-2,3-双加氧酶诱导的肿瘤血管生成，可用作退烧药和止疼剂。

Kinesore是一种细胞可渗透的小分子调节剂，主要与微管马达蛋白kinesin-1结合,从而抑制KLC2（驱动蛋白轻链2）和SKIP（SKIP蛋白）之间的相互作用，从而调节微管网络的结构来影响细胞骨架的组织和动力学。

RKI1313 (RKI-1313) 是一种选择性抑制剂，可抑制 ROCK 依赖性信号传导、细胞骨架变化、不依赖锚定的集落形成、迁移和侵袭。

AA-BR-157 是一种 PROTAC 降解剂，能够降解金属硫蛋白 2A (MT2A)，其 DC50 为 190 nM。同时，AA-BR-157 可下调细胞骨架及细胞运动调节蛋白 DIAPH3，并在 MDA-MB-231 和 U-87 MG 细胞中抑制细胞迁移。此外，AA-BR-157 还可以在 MDA-MB-231 细胞中调节锌稳态。(Pink: ligand for target protein MT2A ligand 1; Black: linker; Blue: ligand for VHL E3 ligase)

AK 275 is a calpain inhibitor that prevents degradation of cytoskeletal and myelin proteins in spinal cord in vitro.

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3 Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB c mice with a dose of 1 mg kg of 3,5-dimethyl PIT-1 per day.

Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membranes, blocking activation.[2] PKC inhibitor peptide is commonly used in cells to evaluate the role of PKC in various cellular responses.[3],[4],[5]

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3,4,5)-P3, also known as PIP3, is resistant to cleavage by PI-specific phospholipase C (PLC). Thus, it is likely to function in signal transduction as a modulator in its own right, rather than as a source of inositol tetraphosphates. PIP3 can serve as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking. PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) is a synthetic analog of natural PIP3 with C6:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacylglycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this analog give it different physical properties from naturally-occurring PIP3, including higher solubility in aqueous media.

The phosphatidylinositol phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3,4,5)-P3 can serve as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains. Centuarin α and the Akt-family of GTPase activating proteins are examples of PtdIns-(3,4,5)-P3-binding proteins. Protein-binding to PtdIns-(3,4,5)-P3 is important for cytoskeletal rearrangements and membrane trafficking. PtdIns-(3,4,5)-P3 is resistant to cleavage by PI-specific phospholipase C (PLC). Thus, it is likely to function in signal transduction as a modulator in its own right, rather than as a source of inositol tetraphosphates. For further reading on inositol phospholipids, see also references and .

Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1 EDG-1, S1P2 EDG-5, S1P3 EDG-3, S1P4 EDG-6, and S1P5 EDG-8. W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 μM (2a = W146; 2b = W140 in supplemental material). It exhibits no biological activity in vivo and can therefore serve as an effective control compound for experiments involving W146.

PF-3758309 dihydrochloride 是一种有效的、可逆的、口服具有活力的、 ATP 竞争性的 PAK4 抑制剂，其 Kd 值为 2.7 nM，Ki 值为 18.7 nM。PF-3758309 dihydrochloride 显示出 PAK4 抑制剂的预期细胞功能，能够抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。

VJ115 is a novel chemical entity that inhibits the enzyme ENOX1, a NADH oxidase. Genetic and small molecule inhibition of ENOX1 inhibits endothelial cell tubule formation and tumor-mediated neo-angiogenesis. Inhibition of ENOX1 radiosensitizes tumor vasculature, a consequence of enhanced apoptosis. VJ115 inhibition of ENOX1 can impact expression of proteins involved in cytoskeletal reorganization and support a hypothesis in which ENOX1 activity links elevated cellular NADH concentrations with cytoskeletal reorganization and angiogenesis.

17(R,S)-Benzo-resolvin D1 (benzo-RvD1) 是专门的分辨介质 (SPM) RvD1 的衍生物。在10和100 nM的浓度下，它能减少PDGF-BB诱导的人类血管平滑肌细胞 (VSMCs) 的细胞骨架变化，并抑制PDGF诱导的这些细胞的迁移。Benzo-RvD1 (10 nM) 抑制人脐静脉内皮细胞 (HUVECs) 中的p65核转位。它还提高了RAW 264.7对S. aureus和zymosan颗粒的吞噬作用。

Sphingosine-1-phosphate (S1P), a bioactive lipid crucial in numerous signaling pathways, undergoes irreversible degradation by membrane-bound S1P lyase, producing (E)-2-Hexadecenal, a derivative of sphingolipid breakdown. This compound can be oxidized to (2E)-hexadecenoic acid by long-chain fatty aldehyde dehydrogenase before being activated through linkage to coenzyme A. Notably, (E)-2-Hexadecenal induces cytoskeletal reorganization, leading to cell rounding, detachment, activation of JNK pathway targets, and ultimate apoptosis in a variety of cell types. Furthermore, it readily forms aldehyde-derived DNA adducts through reactions with deoxyguanosine and DNA.

(E)-2-Hexadecenal alkyne is a click chemistry probe derivative of the sphingolipid degradation product (E)-2-hexadecenal. This compound has demonstrated the ability to induce cytoskeletal reorganization, leading to cell rounding, detachment, activation of downstream JNK targets, and apoptosis in various cell types. Furthermore, it readily reacts with deoxyguanosine and DNA, forming aldehyde-derived DNA adducts.

Nocarnickelamides B (Compound 2) 是一种线性肽类ROCK1 2抑制剂，对ROCK1和ROCK2的IC50值分别为14.9 μM和21.9 μM。其通过结合于ATP结合位点发挥作用，抑制ROCK调控的细胞骨架收缩标志物（如肌球蛋白轻链的激活）。Nocarnickelamides B 在青光眼研究中具备应用潜力。