Rac1 Inhibitor V

A cell-permeable {piperidinylsulfonylphenyl}-pyrazolocarboxamide compound that inhibits celluar Rac-GTP level upon PDGF-BB stimulation (Cat. No. 521225; 20 ng/mL for 2 min) in 48 h 0.4% FCS-starved A617 human vascular smooth muscle cell (SMC) cultures with a higher potency (IC₅₀ = 8.7 µM; 4 h drug preincubation) than Z62954982 (Cat. Nos. 553511 & 553512; 37% inhibition at 50 µM) via a similar mode of action as NSC23766 (Cat. Nos. 553502 & 553508), exhibiting no potency against cellular RhoA-GTP level even at a high concentration of 25 µM. Effectively inhibits SMC adhesion (IC₅₀ = 8.7 µM post 4 h drug treatment) and PDGF-BB-stimulated lamellipodia formation (complete inhibition with 4 h 10 µM; drug treatment prior to 10 min 10 ng/mL PDGF-BB stimulation) of 48 h starved A617 cells. Effectively inhibits Rac activation mediated by Rac-specific Tiam-1 & TrioN GEF as well as non-Rac-specific GEF Vav2, while EHop-016 (Cat. No. 553513), in comparison, is selective against Vav2- over Tiam-1-mediated Rac activation.

Cell permeable: yes

Primary Target
Rac

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Ferri, N., et al. 2013. Med. Chem. Commun.4, 537.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)