a-actin-1

Myosin V-IN-1是一种有效且具有选择性的 Myosin V 抑制剂，Ki 值为 6 μM。Myosin V-IN-1 抑制肌动蛋白 V 发生作用， 通过选择性抑制肌动球蛋白复合物释放 ADP 来减缓肌动蛋白激活的肌球蛋白 V ATP 酶。

AP-1 NF-κB activation inhibitor 1 是一种有效的 AP-1和 NF-κB 介导的转录激活抑制剂(IC50=1 μM)，不阻断 β-actin 启动子驱动的基础转录。AP-1 NF-κB activation inhibitor 1 对受刺激细胞中 IL-2和 IL-8的产生水平有相似的抑制作用。

Ac-Ala-OH (N-Acetyl-L-alanine) 是鸟嘌呤核苷酸结合蛋白G(I) G(S) G(O) γ -2亚基、髓鞘碱性蛋白、GTP-结合核蛋白 Ran、原肌球蛋白 α - 4链、HIV-1 Rev 结合蛋白2、Xaa-Pro 二肽酶、胸腺酶 β -10、肌动蛋白样蛋白3、丙氨酸转氨酶、丝氨酸 苏氨酸蛋白磷酸酶PP1 - β催化亚基、10 kda 热休克蛋白(线粒体)、钙调蛋白和 β -1-syntrophin 的底物。

BRM BRG1 ATP Inhibitor-1 是变构双 Brahma 同源物 (BRM) SWI SNF 相关的基质相关肌动蛋白依赖性调节剂，染色质亚家族 A 成员 2 和 BRG1 SMARCA4 ATP 酶活性抑制剂，IC50值低于 0.005 μM。

Cytochalasin A is a cell-permeable fungal toxin and is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50 = 3 μM), inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhy

ALK5-IN-82 是一种激活素受体样激酶 5 (ALK5) 的高选择性抑制剂，其IC50值仅为 9.1 nM。该化合物能够有效抑制转化生长因子-β 在人脐静脉内皮细胞中诱导的 α-平滑肌肌动蛋白 (α-SMA)、胶原蛋白 I 以及金属蛋白酶抑制剂 1 (TIMP-1) 和基质金属蛋白酶 13 (MMP‐13) 的表达。因此，ALK5-IN-82 有潜力应用于心脏纤维化的相关研究。

IMM-01 是一类新型的哺乳动物透明 (mDia) 相关形式的小分子激动剂，其作用于 Rho GTPase 下游以组装肌动蛋白丝，并与微丝组织在迁移和不对称分裂过程中建立和维持细胞极性. GTP 结合的 Rho 通过破坏 DID 和 DAD 自动调节结构域之间的相互作用来激活 mDia 家族成员，从而释放 FH2 结构域以调节肌动蛋白和微管动力学。

19-O-Acetylchaetoglobosin A is a fungal metabolite originally isolated fromC. globosumthat has actin polymerization inhibitory and cytotoxic activities.1,2It inhibits actin polymerization in a cell-free assay when used at a concentration of 2 μM.219-O-Acetylchaetoglobosin A (3.2, 10, and 32 μg ml) is cytotoxic to HeLa cervical cancer cells.1 1.Umeda, M., Ohtsubo, K., Saito, M., et al.Cytotoxicity of new cytochalasans from Chaetomium globosumExperientia31(4)435-438(1975) 2.Sekita, S., Yoshihira, K., Natori, S., et al.Structure-activity relationship of thirty-nine cytochalasans observed in the effects on cellular structures and cellular events and on actin polymerization in vitroJ. Pharmacobiodyn.8(11)906-916(1985)

Cucurbitacin IIA (Dihydrocucurbitacin Q1) 是从园果雪胆中分离得到的一种三萜烯，可诱导细胞凋亡和增强自噬，有助于葫芦素IIA 对炎症相关疾病的抗炎活性。它可降低癌细胞中生存素的表达，降低磷酸化组蛋白 H3 的水平，增加裂解的 PARP 的水平。

alpha-Cyperone (α-Cyperone) 与 IL-6, Cox-2, Cdc42, Nck-2, Rac1 的表达下调相关,从而能够抑制炎症反应。

The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smooth muscle cell) proliferation and migration in vitro and in neointimal formationin vivo[3]. CGP 53716 inhibited serum-induced cell growth in RASMC (rat aortic smooth muscle cells). And it completely blocked PDGF-BB tyrosine receptor autophosphorylation in RASMC and 3T3 cells, PDGF-BB-induced phosphorylation of mitogen-activated protein kinase at 1 μM in RASMC and inhibited PDGF-BB-induced c-Fos protein expression at 1 μM in RASMC; consistent with inhibition of PDGF-BB-induced DNA synthesis. Further, CGP 53716 inhibited PDGF-BB-, bFGF- and EGF-induced DNA synthesis in a concentration-dependent manner in each cell line. And it showed a 2- to 4-fold selectivity for PDGF-BB-stimulated DNA synthesis over bFGF or EGF in RASMC or 3T3 cells[1]. CGP 53716 inhibited dose dependently tyrosine phosphorylation of both the known PDGFRs: the PDGFR-α and PDGFR-β. After rat carotid artery ballooning injuryin vivo, the migration of alpha-actin-positive cells on the luminal side of internal elastic lamina was decreased with 50 mg kg day of CGP 53716 from 38 ± 10 (control group) to 4 ± 2. Intima media ratio was inhibited by 40% after 14 days in the CGP 53716-treated group (P=0.028) after rat aortic denudation[3].

Y27632 is a selective ROCK inhibitor, which inhibits ET-1-induced increases in natriuretic peptide production, cell size, protein synthesis, and myofibrillar organization. Y27632 prevents dimethylnitrosamine-induced hepatic fibrosis in rats, increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium, affects initial heart myofibrillogenesis in cultured chick blastoderm, promotes the proliferation and cell cycle progression of cultured astrocyte from spinal cord.

Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and​ or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudil produced large reductions in IOP in rabbits and monkeys that were sustained for at least 24 h after once daily dosing, with transient, mild hyperemia observed as the only adverse effect.

Aplyronine A是具有特异性肌动蛋白解聚活性、抗肿瘤及促凋亡功能的化合物，适用于癌症、肌肉收缩、细胞运动和细胞分裂等研究领域。

187-1, N-WASP inhibitor TFA，一种14-aa 环肽及N-WASP 抑制剂，能有效阻止由磷脂酰肌醇 4,5-二磷酸酯 (PIP2) 触发的肌动蛋白装配，IC50 值达 2 μM。该化合物通过维持蛋白质自身的抑制状态，进而抑制N-WASP 激活Arp2 3 复合体。

LQVTDSGLYRCVIYHPP（LP17）是一种多肽和TREM-1(Triggering Receptor Expressed on Myeloid cells 1)抑制剂，序列来源于小鼠和人类TREM-1和TLT-1胞外结构域之间的高度保守序列，通过类似于诱饵受体的机制抑制肌动蛋白激活TREM-1，具有可穿透大脑屏障的优点，能够减轻神经元损伤和炎症反应。

Azurin (50-77)是一种含铜细菌蛋白azurin的肽段，存在于P. aeruginosa中，具有细胞周期停滞、抑制癌细胞增殖和调节血管生成活性。作为VEGFR2的抑制剂（IC20约为10.7 µM），Azurin (50-77)（20 µM）能在MCF-7乳腺癌细胞中诱导G2 M期的细胞周期停滞。在50 µM的浓度下，减少MCF-7和ZR-75-1乳腺癌细胞的增殖。Azurin (50-77)以25 µM的浓度减少VEGF-A诱导的毛细管管腔形成（IC50 = 12 µM），降低人脐静脉内皮细胞（HUVECs）中与细胞膜相关的F-actin、焦点粘附激酶（FAK）和paxillin的水平，并增加胞外的血小板内皮细胞粘附分子-1（PECAM-1）的水平。在体内，Azurin (50-77)（每日10 mg kg）在MCF-7小鼠异种移植模型中减少肿瘤体积。

Tat-Gap 19是一种针对连接蛋白43 (Cx43) 半通道的肽抑制剂，由HIV-1 Tat蛋白传导域与对应于Cx43第128-136残基的九氨基酸肽连接而成。Tat-Gap 19 (10 µM) 能够抑制初级大鼠肝细胞中由谷氨酸引发的ATP释放，这是Cx43半通道活性的标志。在通过中脑动脉堵塞(MCAO)诱导的小鼠脑缺血再灌注损伤模型中，以25 mg/kg的剂量进行给药，可减少梗死体积。腹腔内注射Tat-Gap 19 (1 mg/kg 每天) 能够减少硫代乙酰胺引起的小鼠肝损伤模型中的纤维化病灶面积及表达α-平滑肌肌动蛋白 (α-SMA) 的肝星状细胞（成纤维细胞的前体）面积，并提高同种小鼠分离的肝细胞中超氧化物歧化酶 (SOD) 活性。

Klotho衍生肽1（KP1）(56-87)是从人类Klotho蛋白质中衍生的肽，具有扰乱TGF-β信号传导的作用。它与TGF-β受体类型1（TGFBR2）和TGF-β受体类型2（TGFBR2；Kds分别为1.41和14.6µM）结合。KP1（10 µg/ml）的预孵育抑制TGF-β在NRK-49F大鼠成纤维细胞中诱导的纤维连接蛋白和α-平滑肌肌动蛋白（α-SMA）水平的增加。在体内，KP1（每天1 mg/kg）选择性地定位于受损的肾脏，并减少血清肌酐和血尿素氮水平，这些是肾功能的标志物，同时也减少了小鼠单侧输尿管阻塞（UUO）和单侧缺血-再灌注损伤诱导的肾脏纤维化模型中的肾纤维化。

15(R)-Prostaglandin D2作为一种潜在的前列腺素DP(2)受体激动剂，展现出抗炎活性。它能促进人嗜酸性粒细胞内肌动蛋白的聚合，同时提高血小板中的cAMP水平。

1,2-Dioleoyl-sn-glycero-3-phospho-(1'-myo-inositol-5'-phosphate) ammonium是一种膜结合的信号分子，能调节细胞内的膜运输和信号转导。它可用于脂质体制备，以提高化合物的传递效率。此外，1,2-Dioleoyl-sn-glycero-3-phospho-(1'-myo-inositol-5'-phosphate) ammonium作为肌动蛋白细胞骨架的协调者，参与细胞形态和运动的调控。

16-epiLatrunculin B, a stereoisomer of the actin polymerization inhibitor latrunculin B, was initially isolated from the Red Sea sponge N. magnifica. At concentrations of 5-10 µg/ml, it disrupts microfilament activity in actin disruption assays and exhibits cytotoxic effects on mouse KA31T and NIH3T3 tumor cells, with GI50 values of 1 and 4 µg/ml, respectively. Furthermore, it shows antiviral activity against herpes simplex type 1 virus, with an ED50 of 1 µg/ml.