SKF-96365
TRPC channel blocker / SKF-96365 (130495-35-1) was originally described as a selective blocker of receptor-mediated calcium entry (RMCE), IC50s= 8.5 and 11.7 µM for ADP- and thrombin-stimulated platelets respectively.1 TRPC channels have been shown to mediate RMCE2 and are believed to be the major target of SKF3. In rat vascular smooth muscle Ca entry was reduced by 10 µM SKF which was attributed to TRPC3.4 It has also been shown to inhibit L-type Ca channels.1 More recently it has been demonstrated to be a potent blocker of LVA hCaV3.1 T-type Ca channels, IC50=563 nM (state independent).5 Thus caution should be exercised when using SKF as a sole agent and appropriate controls are recommended.
Biochemicals & reagents
130495-35-1
1 Merritt et al., (1990) SKF96365, a novel inhibitor of receptor-mediated calcium entry; Biochem.J. 271 515 2 Clapham et al., (2001) The TRP ion channel family; Nat. Rev. Neurosci. 2 515 3 Zhu et al., (1998) Receptor-activated Ca2+ influx via human Trp3 stably expressed in human embryonic kidney (HEK)293 cells. Evidence for a non-capacitive Ca2+ entry; J. Biol. Chem. 273 133 4 Liu et al., (2009) Increased transient receptor potential canonical type 3 channels in vasculature from hypertensive rats Hypertension 53 70 5 Singh et a, (2010) The transient receptor potential channel antagonist SKF96365 is a potent blocker of low-voltage-activated T-type calcium channels; Br.J.Pharmacol. 160 1464
RT
TARGET: Ion channel -- PATHWAY: Calcium signaling; Coagulation; Cell cycle; MAPK; Cation channel -- DISEASE AREA: Cancer