YKL-06-061

YKL-06-061 is an inhibitor of salt-inducible kinase 1 (SIK1), SIK2, and SIK3 (IC50s = 6.56, 1.77, and 20.5 nM, respectively). It is selective for these SIKs over a panel of 468 additional kinases at 1 µM but does inhibit FRK, CSF1R, p38alpha, p38beta, EphB1, and TNK2 (IC50s = 1.1, 9.66, 10.1, 9.64, 16.4, and 10.5 nM, respectively) and to a lesser extent KIT, Src, BRK, PDGFRbeta, and NLK (IC50s = 153, 58.8, 24.1, 103, and 132 nM, respectively). YKL-06-061 (37.5 mM) induces pigmentation in human breast skin explants. In vivo, YKL-06-061 (20 mg/kg) decreases seizure severity in a mouse model of epilepsy induced by pentylenetetrazole (PTZ, Cay-18682).Formal Name: 1-cyclobutyl-3-(2,6-dimethylphenyl)-3,4-dihydro-7-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-pyrimido[4,5-d]pyrimidin-2(1H)-one. CAS Number: 2172617-15-9. Molecular Formula: C30H37N7O2. Formula Weight: 527.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml, Chloroform: Sparingly soluble: 1-10 mg/ml. SMILES: CN1CCN(C2=CC(OC)=C(NC3=NC=C(CN4C5=C(C=CC=C5C)C)C(N(C4=O)C6CCC6)=N3)C=C2)CC1. InChi Code: InChI=1S/C30H37N7O2/c1-20-7-5-8-21(2)27(20)36-19-22-18-31-29(33-28(22)37(30(36)38)23-9-6-10-23)32-25-12-11-24(17-26(25)39-4)35-15-13-34(3)14-16-35/h5,7-8,11-12,17-18,23H,6,9-10,13-16,19H2,1-4H3,(H,31,32,33). InChi Key: GVBAXIVNAHMIGH-UHFFFAOYSA-N.