actin polymerization

Wiskostatin is a selective inhibitor of N-WASP, a ubiquitously expressed member of the Wiskott-Aldrich Syndrome protein (WASp) family that regulates actin polymerization.

Aminopurvalanol A is a competitive, selective and cell-permeable inhibitor of cyclin-dependent kinase (CDK) that potently inhibits Cyclin A/cdk2, Cyclin B/cdk1, Cyclin E/cdk2, and P35/cdk5 with IC50 of 33 nM, 33 nM, 28 nM and 20 nM, respectively.

Adriforant (PF-3893787,ZPL-3893797) is a competitive H4 (histamine receptor 4) antagonist that antagonizes histamine-induced phosphorylation of ERK, normalizes histamine-induced transcriptional changes in mast cells and reduces histamine-dependent Ca2+ fluxes in neurons, which alleviates itching and skin inflammation in mice

Benproperine phosphate (Pirexyl phosphate) is a cough suppressant.

Cytochalasin A, a cell-permeable fungal toxin and oxidized derivative of cytochalasin B, is an inhibitor of HIV-1 protease (IC50 = 3 μM). It inhibits actin polymerization, interferes with microtubule assembly by reacting with sulfhydryl groups, and serves as an antibiotic and bactericidal active agent.

Jasplakinolide(Jaspamide), a naturally occurring cyclic peptide from marine sponges, is a potent inducer of actin polymerization.Jasplakinolide exhibits antifungal and antitumor activity and stabilizes pre-existing actin filaments. Jasplakinolide competitively binds to F-actin with the ghost pen cyclic peptide and has a Kd value of 15 nM for F-actin.

Resolvin D1 (RvD1) is an endogenous pro-inflammatory mediator that blocks pro-inflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α-mediated inflammation in macrophages, and enhances macrophage phagocytosis of apoptotic cells.

Latrunculin A is a toxin isolated from the red sea sponge Latrunculia magnifica. Latrunculin A binds to actin monomers and it also inhibits polymerization of actin (Kds: 0.1, 0.4, 4.7 μM, and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin, and G-actin, re

CK-636 (CK-0944636), an Arp2/3 complex inhibitor, can inhibit actin polymerization induced by the human (IC50: 4 μM), fission yeast (IC50: 24 μM) and bovine (IC50: 32 μM) Arp2/3 complex, respectively.

Latrunculin B, an alkaloid from the Red Sea sponge, is an actin polymerization inhibitor with antifungal and antiprotozoal activity.Latrunculin B modulates the electrophysiological characteristics of the pulmonary veins and attenuates the occurrence of torsade de pointes, and may be used in the study of glaucoma in adolescents.

GTPγS (Guanosine 5'-[γ-thio]triphosphate) acts as a G protein activator, protecting proteins from proteolytic degradation. It stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, enhances phospholipase activity, and induces actin polymerization. The combination of GTPγS and G protein α is useful for studying kinase activity. Additionally, GTPγS can be included as a component of lysis buffers.

SMIFH2 is formin homology 2 (FH2) domains inhibitor.

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)

Diminutol is a cell-permeable purine derivative that inhibits the NADP-dependent oxidoreductase, NQO1 (Ki = 1.72 μM), to destabilize microtubules and disrupt mitosis. At 50 μM, it directly affects tubulin polymerization in Xenopus egg extracts without interfering with the activity of Cdk1, DNA replication, or actin polymerization.

Kibdelone C is a member of a family of natural heterocyclic polyketides first isolated from a soil actinomycete, Kibdelosporangium. Kibdelones have been described as having potent and selective cytotoxicity against a panel of human tumor cell lines, and kibdelone C has low nanomolar effectiveness in these assays. Kibdelone C disrupts the actin cytoskeleton without directly binding actin or affecting its polymerization in vitro.

1. alpha-Cyperone (α-Cyperone) is a promising inhibitor of Hla production by S. aureus and protects lung cells from this bacterium. 2. alpha-Cyperone significantly inhibited PGE2 production by suppressing the LPS-induced expression of inducible COX-2 at both the mRNA and the protein levels , downregulated the production and mRNA expression of the inflammatory cytokine IL-6. 3. alpha-Cyperone inhibited actin cytoskeleton polymerization induced by APEC-O78 through down regulating the expression of Nck-2, Cdc42 and Rac1.

Fluvoxketone is trifluoromethyl-substituted aryl ketone compound useful as an intermediate in the synthesis of Fluvoxamine, which is a selective serotonin reuptake inhibitor. In the synthesis of Fluvoxamine, the ketone carbonyl of Fluvoxketone is elaborated to an oxime.In vitro，the inhibitory effect of fluvoxamine on actin polymerization was concentration dependent, and its IC50 was approximately 30 μM.In vivo，fluvoxamine treated EAE rats showed a decrease in IFN-γ serum levels and an increase in IL-4, pro- and anti-inflammatory cytokines respectively.

DMGF, also known as 7,7-dimethoxyagastisfavone, is a biflavonoid isolated from Taxus × media cv. Hicksii. DMGF induces apoptotic and autophagic cell death. DMGF could effectively attenuate the motility of B16F10 cells, and the results of real-time PCR revealed that DMGF also suppressed the expressions of matrix metalloproteinase-2 (MMP-2). MGF can inhibit the metastasis of highly invasive melanoma cancer cells through the down-regulation of F-actin polymerization DMGF may be further developed to serve as a chemoprevention drug for patients with metastatic melanoma.

EG-011 is a first-in-class and potent activator of Wiskott-Aldrich syndrome protein (WASP) that relieves autoinhibition of WASP and robustly induces actin polymerization, EG-011 exhibits selective antitumor activity in lymphomas, supporting its use in cancer biology research to investigate cytoskeletal regulation, immune cell signaling, and WASP-driven tumor vulnerabilities.

AuM1Phe, an N-heterocyclic carbene (NHC) metal complex, inhibits both human topoisomerase I activity and actin polymerization. It also impedes the proliferation of MDA-MB-231 breast cancer cells, exhibiting an IC50 value of 1.2 μM [1].

Histatin 3, a salivary antimicrobial peptide, exhibits activity against C. albicans with an LC50 of 9.2 µM. Additionally, at a concentration of 12 µM, it promotes actin polymerization in cell-free assays.

15(R)-Prostaglandin D2 functions as a DP(2) receptor (Prostaglandin Receptor) agonist with potential roles in prostatic hormone signaling and exhibits anti-inflammatory properties. It enhances actin polymerization in human eosinophils and elevates cAMP levels in platelets [1].

alpha-Cyperone (Standard) is a reference standard for research and analysis in studies involving alpha-Cyperone. 1. alpha-Cyperone (α-Cyperone) is a promising inhibitor of Hla production by S. aureus and protects lung cells from this bacterium. 2. alpha-Cyperone significantly inhibited PGE2 production by suppressing the LPS-induced expression of inducible COX-2 at both the mRNA and the protein levels , downregulated the production and mRNA expression of the inflammatory cytokine IL-6. 3. alpha-Cyperone inhibited actin cytoskeleton polymerization induced by APEC-O78 through down regulating the expression of Nck-2, Cdc42 and Rac1.

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.