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。

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。

Phalloidin 是一种在鹅膏菌中发现的双环七肽，能与 F-肌动蛋白特异性结合，稳定微丝并抑制其解聚，从而干扰细胞的运动和生长。Phalloidin 本身不具有荧光，常与荧光分子偶联后用于 F-肌动蛋白染色，广泛应用于细胞骨架成像以及脑血管标记等研究。

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)

TR-100是一种靶向肿瘤相关原肌球蛋白的小分子抑制剂，可特异性结合Tropomyosin 3.1的C末端，从而干扰其与肌动蛋白丝的相互作用并削弱细胞骨架稳定性。TR-100可选择性影响癌细胞中依赖Tpm3.1的肌动蛋白丝功能，而对正常组织(如心肌)影响较小，主要用于研究肿瘤细胞增殖、迁移及存活相关机制。此外，TR-100对Dynamin-1具有抑制作用，IC50值为10.8 µM。

DHI1 是一种抗白血病剂，在 Jurkat (IC50= 21.83 μM) 和 HL-60 (IC50= 19.14 μM) 白血病细胞中显示出高选择性，同时对非癌细胞的毒性较低。它能诱导 Jurkat 和 HL-60 细胞的 G2/M 细胞周期停滞，以及 HL-60 细胞的 S 期停滞，并对细胞周期信号分子 Wee1, cyclin B1, cdc2 on Tyr15, Chk1 有显著影响。通过破坏细胞骨架中的肌动蛋白丝，DHI1 抑制了 Jurkat 和 HL-60 细胞的迁移与侵袭性，可用于血液恶性肿瘤研究。

20:4 Lyso PI 是一种G蛋白偶联受体GPR55的选择性激动剂。在表达GPR55的HEK293细胞中，其EC50值为10 nM，可以诱发细胞的圆化。20:4 Lyso PI 促进RhoA的激活以及随后的ROCK依赖的细胞骨架重排，同时激活ERK信号通路并提升细胞内游离钙水平。此化合物可用于免疫疾病的研究。

E8431是一种DCSTAMP拮抗剂，DCSTAMP是协调破骨细胞生成过程中细胞-细胞融合的关键融合蛋白。E8431通过抑制RAP1B-RAC1信号通路导致的细胞骨架重组，能够抑制破骨细胞的前融合，并同时抑制骨吸收和刺激PDGFBB的分泌，从而促进骨和血管的生成。E8431有效减轻卵巢切除引起的小鼠模型骨丢失，可用于骨质疏松症的研究。

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

Pfn1-IN-C1是一种靶向Profilin-1(Pfn1)的抑制剂，可干扰其与肌动蛋白的结合，从而扰乱肌动蛋白聚合及细胞骨架动态重构。通过阻断Pfn1-Actin相互作用，Pfn1-IN-C1能够降低内皮细胞的血管生成能力，常用于研究细胞迁移及血管生成相关机制。

PT-262 是一种高效的 Rho 相关蛋白激酶（ROCK）抑制剂，其 IC50 约为 5 μM。PT-262 可诱导线粒体膜电位丧失，增强 caspase-3 的激活并促进细胞凋亡，同时通过不依赖 p53 的信号通路抑制 ERK 和 CDC2 的磷酸化，破坏细胞骨架组织和细胞迁移，从而整体上发挥广泛的抗肿瘤活性，是机制性肿瘤生物学和信号转导研究中的重要工具。

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.

Epsilon-V1-2 是蛋白激酶 C ε（PKCε）的特异性抑制剂。Epsilon-V1-2 被用于卵巢衰老、人颗粒细胞凋亡、脑缺血-再灌注损伤、脑发育、肝细胞胰岛素信号转导以及缺血条件下神经元细胞死亡等相关研究。研究表明，Epsilon-V1-2 能够有效降低 PKCε 的活性，从而促进对线粒体动力学、钙超载、AKT 激活、脑萎缩、胰岛素抵抗及铁死亡等调控通路的深入解析。Epsilon-V1-2 在卒中、SHORT 综合征、肝脂肪变性及脑损伤等疾病模型中显示出显著的治疗相关性。

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.

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。

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.