Arp2/3 Complex Inhibitor

Cytochalasin D (Zygosporin A) is a potent actin polymerization inhibitor, could be derived from fungus. Cytochalasin D has cell-permeable activity. Cytochalasin D inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells. Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of Yap.

CK-666 is a cell-permeable actin-related protein Arp2/3 complex inhibitor (IC₅₀=12 μM). CK-666 binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation.

SMIFH2 is a formin specific inhibitor. SMIFH2 inhibits actin polymerization by Formins and affects the actin cytoskeleton.

Latrunculin A (LAT-A), found in the red sea sponge Latrunculia magnifica, is a G-actin polymerization inhibitor. Latrunculin A binds to actin monomers and inhibits polymerization of actin with K_ds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively. Latrunculin A has effective anti-metastatic properties for cancer research. Latrunculin A blocks cell migration.

Myelin Basic Protein (Porcine), the second most abundant protein in central nervous system myelin, is responsible for adhesion of the cytosolic surfaces of multilayered compact myelin. Myelin Basic Protein (Porcine) mediates interactions with actin and tubulin and effect of post-translational modifications.

CK-869 is an Actin-Related Protein 2/3 (ARP2/3) complex inhibitor, with an IC₅₀ of 7 μM.

Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization by stabilization of the closed, autoinhibited conformation, thereby preventing Arp2/3 complex activation. Wiskostatin is also a dynamin inhibitor with an IC₅₀ value of 20.7 μM and a potent inhibitor of clathrin-mediated endocytosis with an IC₅₀ value of 6.9 μM. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels. Wiskostatin also induces disassembly of podosomes in a murine monocyte cell line.

Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis.

CK-636 is a cell permeable inhibitor of Arp2/3 complex, that could inhibit actin polymerization, with IC₅₀ values of 4 μM, 24 μM and 32 μM for human, fission yeast and bovine, respectively. CK636 blocks cell migration.

NSC305787 is an inhibitor of ezrin with a K_d of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC₅₀ of 8.3 μM, has antitumor activity.

NSC305787 hydrochloride is an inhibitor of ezrin with a K_d of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC₅₀ of 8.3 μM, has antitumor activity.

BDP-13176 is a potent fascin 1 inhibitor, with a K_d of 90 nM and an IC₅₀ of 240 nM. BDP-13176 has potential as an anti-metastatic agent.

TR-100 is a small molecule inhibitor of tumor-associated troponin (Tpm). TR-100 affects the interaction of Tpm3.1 with actin filaments by binding to the C-terminal of Tpm3.1, thereby affecting the stability and function of the actin filaments. This mechanism of action allows TR-100 to specifically affect actin filaments in cancer cells without compromising heart muscle function. TR-100 can be used to study the role of Tpm3.1 in cancer cell proliferation and survival and the effects of Tpm3.1 on insulin-stimulated glucose uptake and insulin secretion.

187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC₅₀ of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.

CK-548 (CK-0993548) is a Arp2/3 complex inhibitor with the IC₅₀ of 11 μM. CK-548 inhibits HIV-1 nuclear migration and infection.

Spire2/FMN2 PPI-IN-1 (Compound 13) is a selective inhibitory fragment targeting the Spire2-FMN2 interaction, with an IC₅₀ of 62 μM. Spire2/FMN2 PPI-IN-1 has affinity for KIND2, with a K_d of 87.7 μM, and does not inhibit KIND1. Spire2/FMN2 PPI-IN-1 can be used for the development of chemical probes for the Spire2-FMN2 interaction.

Spire2/FMN2 PPI-IN-1 (Compound 13) dihydrochloride is a selective inhibitory fragment targeting the Spire2-FMN2 interaction, with an IC₅₀ of 62 μM. Spire2/FMN2 PPI-IN-1 dihydrochloride has affinity for KIND2, with a K_d of 87.7 μM, and does not inhibit KIND1. Spire2/FMN2 PPI-IN-1 dihydrochloride can be used for the development of chemical probes for the Spire2-FMN2 interaction.

PLH1215 is a compound used to regulate, limit, or inhibit the expression of AVIL (advillin), which can be utilized in cancer research.

19-O-Acetylchaetoglobosin A, a cytochalasan alkaloid, is a fungal metabolite originally isolated from C. globosum that has actin polymerization inhibitory and cytotoxic activities. 19-O-Acetylchaetoglobosin A is cytotoxic to HeLa cervical cancer cells.

187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC₅₀ of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.