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Actin Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Arp2/3 Complex (7) Akt (1) Antibiotic (2) Apoptosis (4) Autophagy (3) Bacterial (1) Cathepsin (1) CDK (1) Dynamin (1) Epigenetic Reader Domain (1) FAK (1) Fungal (3) HIV Integrase (1) HIV Protease (1) LIM Kinase (LIMK) (1) MMP (1) Myosin (2) NF-κB (3) Parasite (1) Phospholipase (2) PI3K (1) PKA (1) Ras (1) ROCK (3) Src (1) YAP (1)
By Research Areas:	Cancer (12) Infection (7) Inflammation/Immunology (9) Metabolic Disease (1) Neurological Disease (3)

Inhibitors & Agonists

Peptides

Natural
Products

Targets Recommended: Arp2/3 Complex

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-16929

Latrunculin A 5+ Cited Publications LAT-A
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 .

HY-16931

SMIFH2

1 Publications Verification

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

SMIFH2 1 Publications Verification
SMIFH2 is a formin specific inhibitor. SMIFH2 inhibits actin polymerization by Formins and affects the actin cytoskeleton .

HY-N6682

Cytochalasin D Maximum Cited Publications 40 Publications Verification Zygosporin A; NSC 209835	Arp2/3 Complex Antibiotic YAP	Infection
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 .

HY-N6772

Cytochalasin E	Autophagy	Cancer
Cytochalasin E, an epoxide containing Aspergillus-derived fungal metabolite, inhibits angiogenesis and tumor growth. Cytochalasin E is a potent actin depolymerization agent, and it binds and caps the barbed end of actin filaments to prevent actin elongation .

HY-114657A

Benproperine phosphate	Arp2/3 Complex	Inflammation/Immunology Cancer
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 .

HY-16927

CK-869

1 Publications Verification

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

CK-869 1 Publications Verification
CK-869 is an Actin-Related Protein 2/3 (ARP2/3) complex inhibitor, with an IC₅₀ of 7 μM.

HY-128971

LHVS	Cathepsin Parasite	Infection Neurological Disease
LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC₅₀ of 10 μM .

HY-101848

Latrunculin B	Fungal	Infection
Latrunculin B, an antimicrobial marine alkaloid, is an actin polymerization inhibitor. Latrunculin B regulates pulmonary vein electrophysiological characteristics and attenuates stretch-induced arrhythmogenesis. Antifungal and antiprotozoal activity .

HY-12534

Wiskostatin 1 Publications Verification	Arp2/3 Complex	Neurological Disease
Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels .

HY-112362

3-(4-Pyridyl)indole Rockout; 3-(4-Pyridinyl)-1H-indole; Rho Kinase Inhibitor III, Rockout	ROCK	Inflammation/Immunology
3-(4-Pyridyl)indole (Rockout) is a Rho-kinase (ROCK) inhibitor, with an IC₅₀ of 25 μM. 3-(4-Pyridyl)indole can inhibit blebbing and cause dissolution of actin stress fibers in a wound healing assay .

HY-15892

CK-636 1 Publications Verification CK-0944636	Arp2/3 Complex	Inflammation/Immunology Cancer
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.

HY-N6773

Cytochalasin A	HIV Protease Fungal	Infection
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC₅₀=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives .

HY-N6744

Chaetoglobosin A	Apoptosis	Infection Cancer
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration .

HY-120213

YH-306	FAK Src PI3K MMP Apoptosis	Cancer
YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization .

HY-104013

Aminopurvalanol A	CDK Apoptosis	Cancer
Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .

HY-151189

ROCK-IN-4	ROCK	Others
ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. ROCK-IN-4 reversibly depolymerizes F-actin, and suppresses mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 can be used for glaucoma or ocular hypertension research .

HY-121750

CCG-222740	Ras ROCK	Cancer
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor . CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis .

HY-152949

Myosin V-IN-1	Myosin	Neurological Disease
Myosin V-IN-1 (compound 8) is a potent and selective Myosin V inhibitor, with a K_i of 6 μM. Myosin V-IN-1 shows acute inhibition of myosin V. Myosin V-IN-1 slows the actin-activated myosin V ATPase by specifically inhibiting ADP release from the actomyosin complex .

HY-123572

Bis-T-23 AG1717	Dynamin HIV Integrase	Infection Metabolic Disease Inflammation/Immunology
Bis-T-23 (AG1717), tyrphostin derivative, is an HIV-I integrase inhibitor. Bis-T-23 can promote actin-dependent dynamin oligomerization. Bis-T-23 can be used for the research of HIV and chronic kidney diseases (CKD) .

HY-16690

BTS 2 Publications Verification N-Benzyl-p-toluenesulfonamide; N-Tosylbenzylamine	Myosin	Others
BTS (N-Benzyl-p-toluenesulfonamide) is a potent and selective inhibitor of skeletal muscle myosin II subfragment 1 (S1) ATPase activity, with an IC₅₀s of ~5 µM for actin- and Ca ²⁺-stimulated myosin S1 ATPase. BTS specifically inhibits the contraction of fast skeletal muscle fibers .

HY-P1045

187-1, N-WASP inhibitor 1 Publications Verification	Arp2/3 Complex	Others
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 .

HY-12807

FIPI 4 Publications Verification 5-Fluoro-2-indolyl deschlorohalopemide	Phospholipase Autophagy	Inflammation/Immunology Cancer
FIPI (5-Fluoro-2-indolyl des-chlorohalopemide), a derivative of Halopemide (HY-119093), is a phospholipase D (PLD) inhibitor with IC₅₀s of approximately 25 nM and 20 nM for PLD1 and PLD2, respectively. FIPI inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. FIPI has the potential for autoimmunity and cancer metastasis research .

HY-12807A

FIPI hydrochloride 5-Fluoro-2-indolyl deschlorohalopemide hydrochloride	Phospholipase Autophagy	Inflammation/Immunology Cancer
FIPI (5-Fluoro-2-indolyl des-chlorohalopemide) hydrochloride, a derivative of Halopemide (HY-119093), is a phospholipase D (PLD) inhibitor with IC₅₀s of approximately 25 nM and 20 nM for PLD1 and PLD2, respectively. FIPI hydrochloride inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. FIPI hydrochloride has the potential for autoimmunity and cancer metastasis research .

HY-N6701

Dihydrocytochalasin B	Arp2/3 Complex	Cancer
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport . Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis . Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca ²⁺increase in the mucosal scrapings .

HY-16926

CK-666 4 Publications Verification
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 .

HY-P1045A

187-1, N-WASP inhibitor TFA	Arp2/3 Complex	Others
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 .

HY-133987

AP-1/NF-κB activation inhibitor 1 1 Publications Verification	NF-κB	Inflammation/Immunology
AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC₅₀=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells .

HY-119374

BRM/BRG1 ATP Inhibitor-1 15+ Cited Publications	Epigenetic Reader Domain	Cancer
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC₅₀s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity .

HY-P5455

S3 Fragment	LIM Kinase (LIMK)	Others
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)

HY-N6727

Gliotoxin Aspergillin	Apoptosis PKA NF-κB Bacterial Fungal Antibiotic	Infection Inflammation/Immunology Cancer
Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis . Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells . Gliotoxin is a potent NOTCH2 transactivation inhibitor, can effectively induce apoptosis of chronic lymphocytic leukemia (CLL) cells .

HY-N6588

3,4,5-Tricaffeoylquinic acid 3,4,5-triCQA	Akt NF-κB	Inflammation/Immunology
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .

187-1, N-WASP inhibitor 1 Publications Verification	Arp2/3 Complex	Others
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 .

187-1, N-WASP inhibitor TFA	Arp2/3 Complex	Others
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 .

S3 Fragment	LIM Kinase (LIMK)	Others
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)

Cytochalasin D 35+ Cited Publications Zygosporin A; NSC 209835	Infection Structural Classification Natural Products Microorganisms Classification of Application Fields Source classification Disease Research Fields	Arp2/3 Complex Antibiotic YAP
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 .

Cytochalasin E	Alkaloids Microorganisms Pyrrole Alkaloids Classification of Application Fields Source classification Disease Research Fields Cancer	Autophagy
Cytochalasin E, an epoxide containing Aspergillus-derived fungal metabolite, inhibits angiogenesis and tumor growth. Cytochalasin E is a potent actin depolymerization agent, and it binds and caps the barbed end of actin filaments to prevent actin elongation .

Latrunculin B	Infection Animals Classification of Application Fields Marine natural products Sponge Disease Research Fields	Fungal
Latrunculin B, an antimicrobial marine alkaloid, is an actin polymerization inhibitor. Latrunculin B regulates pulmonary vein electrophysiological characteristics and attenuates stretch-induced arrhythmogenesis. Antifungal and antiprotozoal activity .

Cytochalasin A	Infection Alkaloids Microorganisms Pyrrole Alkaloids Classification of Application Fields Source classification Disease Research Fields	HIV Protease Fungal
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC₅₀=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives .

Chaetoglobosin A	Infection Alkaloids Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Source classification Marine natural products Endogenous metabolite Disease Research Fields Marine microorganism Indole Alkaloids	Apoptosis
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration .

Gliotoxin Aspergillin	Structural Classification Anti-inflammation/Immunoregulatory Classification of Application Fields Source classification Antibacterial Disease Research Other Antibiotics Biological Pesticide Research Agricultural Research Infection Microorganisms Antibiotics Inflammation/Immunology Disease Research Fields	Apoptosis PKA NF-κB Bacterial Fungal Antibiotic
Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis . Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells . Gliotoxin is a potent NOTCH2 transactivation inhibitor, can effectively induce apoptosis of chronic lymphocytic leukemia (CLL) cells .

3,4,5-Tricaffeoylquinic acid 3,4,5-triCQA	Classification of Application Fields Simple Phenylpropanols Source classification Phenols Polyphenols Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields Convolvulaceae Ipomoea batatas (Linn.) Lamarck	Akt NF-κB
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases .

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Actin Inhibitors

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