LJH685

LJH685 is an inhibitor of p90 ribosomal S6 kinases (RSKs, also known as MAP kinase-activated protein kinases, or MAPKAPKs) that inhibits RSK1, 2, and 3 in vitro with IC50 values of 6, 5, and 4 nM, respectively. It is selective for RSKs over a panel of 96 other kinases. LJH685 blocks RSK activity in cells, preventing phosphorylation of y-box-binding protein 1 on Ser102. The inhibition of RSK activity correlates with antiproliferative effects in MAPK pathway-dependent cancer cell lines, but only in an anchorage-independent growth setting.Formal Name: 2,6-difluoro-4-[4-[4-(4-methyl-1-piperazinyl)phenyl]-3-pyridinyl]-phenol. CAS Number: 1627710-50-2. Molecular Formula: C22H21F2N3O. Formula Weight: 381.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:7): 0.125 mg/ml, Ethanol: 2.5 mg/ml. lambdamax: 237, 270, 316 nm. SMILES: CN(CC1)CCN1C(C=C2)=CC=C2C3=CC=NC=C3C4=CC(F)=C(O)C(F)=C4. InChi Code: InChI=1S/C22H21F2N3O/c1-26-8-10-27(11-9-26)17-4-2-15(3-5-17)18-6-7-25-14-19(18)16-12-20(23)22(28)21(24)13-16/h2-7,12-14,28H,8-11H2,1H3. InChi Key: IKUFKDGKRLMXEX-UHFFFAOYSA-N.