Formulation: A solid
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
Purity: ≥98%
Formula Markup: C32H34ClN7O3
Formula Weight: 600,1
Shelf life (days): 1460
CAS Number: 1936529-65-5
Notes: YKL-05-099 is an inhibitor of salt-inducible kinase 2 (SIK2; IC50 = 0.04 µM for the human enzyme).{68145} 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-α, IL-6, and IL-12p40 levels and increases IL-1β 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).{68146} 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.{68147}
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