ATN-161 (Ac-PHSCN-NH2)

For research use only.

Catalog No.S8454

2 publications

ATN-161 (Ac-PHSCN-NH2) Chemical Structure

CAS No. 262438-43-7

ATN-161 (Ac-PHSCN-NH2) is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.

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Selleck's ATN-161 (Ac-PHSCN-NH2) has been cited by 2 publications

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Biological Activity

Description ATN-161 (Ac-PHSCN-NH2) is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
Targets
integrin α5β1 [1]
()
αvβ3 [1]
()
In vitro

ATN-161 interacts with the N-terminus of the β1-domain of integrin α5β1, which may lock this integrin in an inactive conformation[2]. ATN-161 treatment up to 100 μmol/L shows no significant effect on tumor cell proliferation compared with the vehicle-treated control group of cells. However, ATN-161 significantly inhibits MAPK phosphorylation with maximal effects observed at 20 μmol/L of ATN-161 after 30 minutes of treatment[1].

In vivo ATN-161 (Ac-PHSCN-NH2), a 5-mer capped peptide derived from the synergy region of fibronectin that binds to α5β1 and αvβ3 in vitro, blocks breast cancer growth and metastasis. Treatment with ATN-161 causes a significant dose-dependent decrease in tumor volume and either completely blocked or caused a marked decrease in the incidence and number of skeletal as well as soft tissue metastases. Treatment with ATN-161 results in a significant decrease in the expression of phosphorylated mitogen-activated protein kinase, microvessel density, and cell proliferation in tumors grown in vivo[1]. ATN-161 is a peptide with a fairly short plasma half-life. compared with the plasma pharmacokinetics of ATN-161, It is cleared from the tumor with much slower kinetics supporting the hypothesis that this peptide exerts its effects through a durable interaction with its target(s)in the tumor[3].

Protocol

Cell Research:

[1]

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  • Cell lines: MDA-MB-231 cells
  • Concentrations: 1-100 μmol/L
  • Incubation Time: 15-60 minutes
  • Method:

    MDA-MB-231 (1 × 106) cells are plated in 100 mm Petri dishes for 24 hours, then serum-starved overnight before treatment with vehicle or ATN-161 (1-100 μmol/L) for different time periods (15-60 minutes). Western blot analyses are carried out using antibodies against focal adhesion kinase, phosphorylated FAK, mitogen-activated protein kinase (MAPK), phosphorylated MAPK, and β-tubulin as previously described. Western blots are detected using enhanced chemiluminescence detection reagents.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: BALB/c nu/nu mice
  • Dosages: 0.05-1 mg/kg/d
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro Water 13 mg/mL (21.75 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 597.64
Formula

C23H35N9O8S

CAS No. 262438-43-7
Storage powder
in solvent
Synonyms N/A
Smiles CC(=O)N1CCCC1C(=O)NC(CC2=CN=CN2)C(=O)NC(CO)C(=O)NC(CS)C(=O)NC(CC(=O)N)C(=O)N

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Integrin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID