2. Cytoskeleton
  3. Actin
  4. β-actin-IN-1

β-actin-IN-1 is a selective and covalent β-actin polymerization inhibitor. β-actin-IN-1 targets Cys272 of β-actin and shows selectivity over α-actin and γ-actin. β-actin-IN-1 inhibits β-actin polymerization and disrupts the actin cytoskeleton in cancer cells, leading to cell migration inhibition as well as cell death. β-actin-IN-1 can be used for the study of osteosarcoma.

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β-actin-IN-1

β-actin-IN-1 Chemical Structure

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β-actin-IN-1 Related Antibodies

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Description

β-actin-IN-1 is a selective and covalent β-actin polymerization inhibitor. β-actin-IN-1 targets Cys272 of β-actin and shows selectivity over α-actin and γ-actin. β-actin-IN-1 inhibits β-actin polymerization and disrupts the actin cytoskeleton in cancer cells, leading to cell migration inhibition as well as cell death. β-actin-IN-1 can be used for the study of osteosarcoma[1].

IC50 & Target[1]

β-Actin

 

In Vitro

β-actin-IN-1 (compound C25) selectively and covalently binds to Cys272 of β-actin at an allosteric site, inhibits β-actin polymerization, and shows high selectivity for β-actin over α-actin and γ-actin[1].
β-actin-IN-1 (0.001-100 μM; 72 h) inhibits the proliferation of osteosarcoma 143B, HOS, SJSA-1, MG63, MNNG/HOS, A549, MGC803 and HCT116 tumor cells with IC50 values of 0.015, 0.042, 0.20, 0.048, 0.043, 1.2, 0.42 and 0.45 μM respectively, and it presents weaker cytotoxicity against normal HEK293T cells with an IC50 of 0.23 μM, leading to a selectivity index of 15.33[1]. β-actin-IN-1 (10-40 nM; 10 days) reduces 143B cell colony formation[1].
β-actin-IN-1 (10-40 nM; 24 h) inhibits 143B cell migration in wound healing and transwell assays[1].
β-actin-IN-1 (10-40 nM; 2 h) disrupts the actin cytoskeleton and reduces phalloidin-stained actin filaments in 143B cells[1].
β-actin-IN-1 (0.1 μM) shows a T1/2 of 3.88 min and a CLint of 541 mL/min/g in human liver microsomes, and a T1/2 of 1.27 min and a CLint of 1656 mL/min/g in mouse liver microsomes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

β-actin-IN-1 Related Antibodies

Cell Viability Assay

Cell Line: HEK293T, 143B, HOS, SJSA-1, MG63, MNNG/HOS, A549, MGC803, HCT116
Concentration: 0.001-100 μM
Incubation Time: 72 h
Result: Showed lower cytotoxicity in normal HEK293T cells (IC50 = 0.23 μM) than in 143B cells (IC50 = 0.015 μM), with a selectivity index of 15.33.
Inhibited the proliferation of osteosarcoma 143B, HOS, SJSA-1, MG63, MNNG/HOS cells and A549, MGC803, HCT116 tumor cells, with IC50 values of 0.015, 0.042, 0.20, 0.048, 0.043, 1.2, 0.42 and 0.45 μM, respectively.

Cell Proliferation Assay

Cell Line: 143B
Concentration: 0.01, 0.02, 0.04 μM
Incubation Time: 10 days
Result: Reduced 143B cell colony formation in a dose-dependent manner.

Cell Migration Assay

Cell Line: 143B
Concentration: 0.01, 0.02, 0.04 μM
Incubation Time: 24 h
Result: Reduced scratch closure rate and the number of migrated 143B cells in a dose-dependent manner. At 0.02 μM, the scratch closure rate was significantly lower than that of the vehicle group, which verified the potent migration inhibitory effect on 143B cells.

Immunofluorescence

Cell Line: 143B
Concentration: 10, 20, 40 nM
Incubation Time: 2 h
Result: Reduced the fluorescence intensity of phalloidin-stained actin filaments.
Caused loss of stress fibers in most exposed cells, indicating disruption of the actin cytoskeleton and loss of the typical motile phenotype.
In Vivo

β-actin-IN-1 (compound C25) (5, 10 mg/kg; i.p.; once daily; for 14 days) has antitumor activity in a 143B osteosarcoma cell-derived xenograft mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice were subcutaneously inoculated with 143B osteosarcoma cells (5 × 106 cells/animal)[1]
Dosage: 5, 10 mg/kg
Administration: Intraperitoneal injection (i.p.); once daily; for 14 consecutive days
Result: Suppressed 143B osteosarcoma xenograft tumor growth. Achieved a tumor growth inhibition (TGI) rate of 66% in the 10 mg/kg/day group, while sorafenib at 30 mg/kg/day achieved a TGI of 74%.
Reduced tumor volume and tumor weight compared with the vehicle group.
Did not cause significant body weight changes during the administration period.
Did not cause significant changes in heart, liver, spleen, lung or kidney weight.
Showed no overt histological abnormalities in heart, liver, spleen, lung or kidney sections according to H&E staining.
Molecular Weight

400.87

Formula

C22H22ClFN2O2
SMILES

FC1=CC=C(NC2=CC=CC(Cl)=C2N(C(C#C)=O)CCC3CCOCC3)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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β-actin-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

β-actin-IN-1Actinβ-actin inhibitorACTBselective β-actin polymerization inhibitorcovalent inhibitorCys272allosteric siteactin cytoskeletonF-actinG-actinABPPCETSADARTSLC-MS/MS143BHOSSJSA-1MG63MNNG/HOSA549MGC803HCT116HEK293Tosteosarcoma143B xenograft modelInhibitorinhibitorinhibit

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