YKL-05-099

YKL-05-099 is an inhibitor of salt-inducible kinase 2 (SIK2, IC50 = 0.04 µM for the human enzyme). It is selective for SIK2 over a panel of 141 kinases at 1 µM but also inhibits 14 other kinases, including SIK3, Ephrin receptors, and Src. YKL-05-099 increases IL-10 production in zymosan A-induced isolated mouse bone marrow-derived dendritic cells (BMDCs, EC50 = 0.46 µM), as well as decreases TNF-alpha, IL-6, and IL-12p40 levels and increases IL-1beta levels in LPS-stimulated BMDCs when used at a concentration of 1 µM. It inhibits the proliferation of MOLM-13 leukemia cells (IC50 = 0.24 µM). In vivo, YKL-05-099 (10 µmol/kg) increases the bone formation rate and number of femoral osteoblasts and decreases the number of femoral osteoclasts in mice.Formal Name: 3-(2-chloro-6-methylphenyl)-3,4-dihydro-7-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-1-(5-methoxy-2-pyridinyl)-pyrimido[4,5-d]pyrimidin-2(1H)-one. CAS Number: 1936529-65-5. Molecular Formula: C32H34ClN7O3. Formula Weight: 600.1. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml, PBS (pH 7.2): insol. lambdamax: 276, 302 nm. SMILES: O=C1N(C2=NC(NC3=C(OC)C=C(C4CCN(CC4)C)C=C3)=NC=C2CN1C5=C(C=CC=C5Cl)C)C6=CC=C(C=N6)OC. InChi Code: InChI=1S/C32H34ClN7O3/c1-20-6-5-7-25(33)29(20)39-19-23-17-35-31(37-30(23)40(32(39)41)28-11-9-24(42-3)18-34-28)36-26-10-8-22(16-27(26)43-4)21-12-14-38(2)15-13-21/h5-11,16-18,21H,12-15,19H2,1-4H3,(H,35,36,37). InChi Key: VQINULODWGEVBB-UHFFFAOYSA-N.