GPCR-Helix 8 Signaling Inhibitor, JF5

A cell-permeable quinolinimine compound that acts as a selective, potent blocker of G-protein coupled receptors (GPCR) that contain a constrained eighth helix (H8). The inhibition is selective and blocks G-protein signaling mediated via G_αq, but not G_α12. A non-orthosteric antagonist of PAR1 (IC₅₀ = 4 µM) that is shown to inhibit PAR1 and CCR-4 induced platelet aggregation without affecting PAR4 mediated aggregation. Shown to inhibit thrombus formation following vascular injury (IC₅₀ ~1 mg/kg). Also acts as a potent, non-competitive blocker of α2A-adrenergic receptors (IC₅₀ = 2.5 µM as shown by a decrease in ³H-yohimbine binding).

Packaged under inert gas

Toxicity: Standard Handling (A)

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

Dowal, L., et al. 2011. Proc. Natl. Acad. Sci. USA108, 2951.

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