Hexa-D-arginine TFA

Names

[ Name ]:
Hexa-D-arginine TFA

Biological Activity

[Description]:

Hexa-D-arginine TFA (Furin Inhibitor II TFA) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine TFA blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo[1][2][3].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Others >> Others

[Target]

Ki: 106 nM (Furin), 580 nM (PACE4) and 13.2 μM (PC1)[3]

[In Vitro]

Hexa-D-arginine effectively blocks Pseudomonas aeruginosa exotoxin A (PEA)-induced cell lysis and is itself noncytotoxic[1].

[In Vivo]

Administration of Hexa-D-arginine (0.1, 1, or 10 nM) to Pseudomonas aeruginosa exotoxin A (PEA)-treated mice (6-week-old FVB and 129/Sv mice) significantly improves their survival rate and also decreases circulating levels of TNF-α[1].

[References]

[1]. Sarac MS, et al. The furin inhibitor hexa-D-arginine blocks the activation of Pseudomonas aeruginosa exotoxin A in vivo. Infect Immun. 2002 Dec;70(12):7136-9.

[2]. Sarac MS, et al. Protection against anthrax toxemia by hexa-D-arginine in vitro and in vivo. Infect Immun. 2004 Jan;72(1):602-5.

[3]. Cameron A, et al. Polyarginines are potent furin inhibitors. J Biol Chem. 2000 Nov 24;275(47):36741-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₈H₇₆F₃N₂₅O₈

[ Molecular Weight ]:
1068.17

Hexa-D-arginine TFA

Names

Biological Activity

Chemical & Physical Properties

Related Compounds