SR 7826

SR 7826 is an inhibitor of LIM kinase 1 (LIMK1, IC50 = 43 nM). It is selective for LIMK1 over Rho-associated kinase 1 (ROCK1) and ROCK2 (IC50s = 6,565 and 5,536 nM, respectively) and a panel of 60 kinases at 1 µM but does inhibit serine/threonine kinase 16 (STK16) by greater than 80% at 1 µM. SR 7826 inhibits the phosphorylation of cofilin induced by hepatocyte growth factor (HGF) in A7r5 cells (IC50 = 470 nM). It reduces the migration and invasion of PC3 prostate cancer cells when used at a concentration of 1 µM. SR 7826 (1 µM) inhibits electric field stimulation-, phenylephrine-, methoxamine-, norepinephrine-, or U-46619-induced contractions of prostate strips isolated from patients with prostate cancer. In vivo, SR 7826 (10 mg/kg, p.o.) increases apical and basal thin spine density of CA1 pyramidal neurons in the hAPP-J20 mouse model of Alzheimer's disease. InChI: InChI=1S/C22H21N5O2/c1-15-13-23-21-19(15)20(24-14-25-21)16-7-9-17(10-8-16)26-22(29)27(11-12-28)18-5-3-2-4-6-18/h2-10,13-14,28H,11-12H2,1H3,(H,26,29)(H,23,24,25) InChIKey: WQAGVQVBDHOHRD-UHFFFAOYSA-N SMILES: O=C(N(CCO)C1=CC=CC=C1)NC2=CC=C(C3=C4C(C)=CNC4=NC=N3)C=C2