Home Cytoskeletal Signaling Integrin antagonist ATN-161

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ATN-161 Integrin antagonist

ATN-161 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 Integrin antagonist Chemical Structure

Chemical Structure

Molecular Weight: 597.64

Purity & Quality Control

Related Products

Signaling Pathway

Integrin Signaling Pathways

Integrin Signaling Pathway

Mechanism of Action

Targets
integrin α5β1 [1] αvβ3 [1]

In vitro
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]. This compound treatment up to 100 μmol/L shows no significant effect on tumor cell proliferation compared with the vehicle-treated control group of cells. However, this chemical significantly inhibits MAPK phosphorylation with maximal effects observed at 20 μmol/L of this compound after 30 minutes of treatment[1].
Cell Research 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.

In Vivo
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 this compound 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 this peptide 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]. It is a peptide with a fairly short plasma half-life. compared with the plasma pharmacokinetics of this compound, 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].
Animal Research Animal Models BALB/c nu/nu mice
Dosages 0.05-1 mg/kg/d
Administration i.v.

References
  • https://pubmed.ncbi.nlm.nih.gov/16985061/
  • https://pubmed.ncbi.nlm.nih.gov/12584749/
  • https://pubmed.ncbi.nlm.nih.gov/18381955/

Chemical Information

Molecular Weight 597.64 Formula

C23H35N9O8S
CAS No. 262438-43-7 SDF Download SDF
Synonyms Ac-PHSCN-NH2
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

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

Water : 10 mg/mL (超声加热十分钟，60℃)

DMSO : 3 mg/mL ( (5.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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