ATN-161 (Ac-PHSCN-NH2)

Catalog No.S8454

For research use only.

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.

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

CAS No. 262438-43-7

Selleck's ATN-161 (Ac-PHSCN-NH2) has been cited by 7 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 (from reference)

Cell Research:

[1]

  • 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]

  • 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 3 years -20°C powder
2 years -80°C in solvent
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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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