ATN-161 - CAS 262438-43-7
Catalog number: 262438-43-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
ATN-161 is a small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for integrin alpha5beta1, thereby preventing integrin alpha5beta1 binding.
Publictions citing BOC Sciences Products
  • >> More
white solid powder
ATN 161; ATN161; Ac-PHSCN-NH2.
Current Developer:
Attenuon Inc./Tactic Pharma, LLC
1.αvβ3 Integrins Mediate Flow-Induced NF-κB Activation, Proinflammatory Gene Expression, and Early Atherogenic Inflammation.
Chen J1, Green J1, Yurdagul A Jr2, Albert P1, McInnis MC1, Orr AW3. Am J Pathol. 2015 Sep;185(9):2575-89. doi: 10.1016/j.ajpath.2015.05.013. Epub 2015 Jul 26.
Endothelial cell interactions with transitional matrix proteins, such as fibronectin, occur early during atherogenesis and regulate shear stress-induced endothelial cell activation. Multiple endothelial cell integrins bind transitional matrix proteins, including α5β1, αvβ3, and αvβ5. However, the role these integrins play in mediating shear stress-induced endothelial cell activation remains unclear. Therefore, we sought to elucidate which integrin heterodimers mediate shear stress-induced endothelial cell activation and early atherogenesis. We now show that inhibiting αvβ3 integrins (S247, siRNA), but not α5β1 or αvβ5, blunts shear stress-induced proinflammatory signaling (NF-κB, p21-activated kinase) and gene expression (ICAM1, VCAM1). Importantly, inhibiting αvβ3 did not affect cytokine-induced proinflammatory responses or inhibit all shear stress-induced signaling, because Akt, endothelial nitric oxide synthase, and extracellular regulated kinase activation remained intact.
2.Pharmacology of the novel antiangiogenic peptide ATN-161 (Ac-PHSCN-NH2): observation of a U-shaped dose-response curve in several preclinical models of angiogenesis and tumor growth.
Doñate F1, Parry GC, Shaked Y, Hensley H, Guan X, Beck I, Tel-Tsur Z, Plunkett ML, Manuia M, Shaw DE, Kerbel RS, Mazar AP. Clin Cancer Res. 2008 Apr 1;14(7):2137-44. doi: 10.1158/1078-0432.CCR-07-4530.
PURPOSE: ATN-161 (Ac-PHSCN-NH(2)) is an integrin-binding peptide that is currently in phase II trials in cancer patients. This peptide has been shown to have antitumor activity in a number of different preclinical models.
3.α5β1 integrin signaling mediates oxidized low-density lipoprotein-induced inflammation and early atherosclerosis.
Yurdagul A Jr1, Green J1, Albert P1, McInnis MC1, Mazar AP1, Orr AW2. Arterioscler Thromb Vasc Biol. 2014 Jul;34(7):1362-73. doi: 10.1161/ATVBAHA.114.303863. Epub 2014 May 15.
OBJECTIVE: Endothelial cell activation drives early atherosclerotic plaque formation. Both fibronectin deposition and accumulation of oxidized low-density lipoprotein (oxLDL) occur early during atherogenesis, and both are implicated in enhanced endothelial cell activation. However, interplay between these responses has not been established. The objective of our study was to determine whether endothelial matrix composition modulates the inflammatory properties of oxLDL.
4.Potential relevance of bell-shaped and u-shaped dose-responses for the therapeutic targeting of angiogenesis in cancer.
Reynolds AR1. Dose Response. 2010 Apr 23;8(3):253-84. doi: 10.2203/dose-response.09-049.Reynolds.
Tumor angiogenesis, the growth of new blood vessels into tumors, facilitates tumor growth and thus represents an attractive therapeutic target. Numerous experimental angiogenesis inhibitors have been characterised and subsequently trialled in patients. Some of these agents have failed to show any substantial activity in patients. In contrast, others have been more successful, but even these provide only a few months extra patient survival. Recent work has focused on understanding the effects of anti-angiogenic agents on tumor biology and has revealed a number of new findings that may help to explain the limited efficacy of angiogenesis inhibitors. Herein, I review the evidence that hormetic dose-responses (i.e. bell-shaped and U-shaped dose-response curves) are often observed with anti-angiogenic agents. Agents reported to exhibit these types of dose-response include: 5-fluorouracil, ATN-161, bortezomib, cisplatin, endostatin, enterostatin, integrin inhibitors, interferon-α, plasminogen activator-1 (PAI-1), rapamycin, rosiglitazone, statins, thrombospondin-1, TGF-α1 and TGF-α3.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Integrin Products

Cyclo (-RGDfK)
(CAS: 161552-03-0)

Cyclo (-RGDfK) is a potent and selective αvβ3 integrin inhibitor.

CAS 1564286-55-0 CWHM-12

(CAS: 1564286-55-0)

CWHM 12 demonstrated high potency against all of the five possible β subunit binding partners (αvβ1, αvβ3, αvβ5, αvβ6 and αvβ8) in in vitro ligand-binding assay...

CAS 455264-31-0 Zaurategrast

(CAS: 455264-31-0)

Zaurategrast is an oral α4-integrin inhibitor. It significantly decreased the capacity of lymphocytes to bind vascular adhesion molecule-1 (VCAM-1) and the expr...

Cilengitide TFA salt
(CAS: 199807-35-7)

Cilengitide TFA salt, is a cyclic Arg-Gly-Asp acid pentapeptide that induces anoikis in angiogenic blood vessels and brain tumor, selectively and potently block...

CAS 91037-65-9 Arg-Gly-Asp-Ser

(CAS: 91037-65-9)

Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. It is a tetrapeptide found on fibronectin, fibrinogen α, and von Wille...

CAS 188968-51-6 Cilengitide (TFA salt)

Cilengitide (TFA salt)
(CAS: 188968-51-6)

Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and ...

CAS 232271-19-1 TR-14035

(CAS: 232271-19-1)

TR14035 blocked the binding of human alpha(4)beta(7) to an (125)I-MAdCAM-Ig fusion protein with IC(50) values of 0.75 nM. TR14035 blocked binding of human alpha...

(CAS: 1333146-24-9)

ILK-IN-1, a ILK inhibitor, has been found to restrain the tumor cell growth through regulating signaling pathways related to oncogenesis and tumor progression. ...

CAS 904763-27-5 ATN-161 trifluoroacetate salt

ATN-161 trifluoroacetate salt
(CAS: 904763-27-5)

ATN-161 trifluoroacetate salt is a beta integrin antagonist with antitumor activity. It is a five -amino-acid peptide derived from the synergy region of fibrone...


GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor which can be used to modify the surface of cardiovascular implants such as vascular grafts to p...

CAS 150915-40-5 Tirofiban hydrochloride monohydrate

Tirofiban hydrochloride monohydrate
(CAS: 150915-40-5)

Tirofiban is a specific nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Tirofiban is an antithrombotic used in the treatment of unstable angina...

CAS 402567-16-2 Firategrast

(CAS: 402567-16-2)

Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous syste...

CAS 262438-43-7 ATN-161

(CAS: 262438-43-7)

ATN-161 is a small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for i...

CAS 344897-95-6 Leukadherin-1

(CAS: 344897-95-6)

Leukadherin-1, also known as LA1, is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1. Leukadherin-1 suppresses hu...

Integrin Antagonists 27
(CAS: 593274-97-6)

Integrin Antagonists 27, as s novel anticancer agent., is a small molecule integrin αvβ3 antagonist.

CAS 180144-61-0 SR121566A

(CAS: 180144-61-0)

SR121566A, a non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, has been shown to block platelet aggregation induced by a wide variety of agonists incl...

CAS 1307293-62-4 ALG1001

(CAS: 1307293-62-4)

ALG1001, also known as Luminate, a first-in-class integrin peptide therapy, is an angiogenesis inhibitors and Integrin alpha 5 beta 1 modulator. A study from Jo...

(CAS: 669076-03-3)

JNJ26076713 is an orally active alpha V integrin antagonist. It may be a potential therapeutic candidate for the treatment of age-related macular degeneration,p...

(CAS: 1320346-97-1)

GLPG-0187 is a small molecule integrin receptor antagonist (IRA) with nanomolar affinity for the RGD-integrin receptors αvβ1, αvβ3, αvβ5, αvβ6 and α5β1 (IC50s =...

Chemical Structure

CAS 262438-43-7 ATN-161

Quick Inquiry

Verification code

Featured Items