An inhibitor of SIK2
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YKL-05-099

Item No. 36116

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): insol
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $160

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    10 mg

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    25 mg

    $519

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    50 mg

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    Product Description

    YKL-05-099 is an inhibitor of salt-inducible kinase 2 (SIK2; IC50 = 0.04 µM for the human enzyme).1 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).2 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.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sundberg, T.B., Liang, Y., Wu, H., et al. Development of chemical probes for investigation of salt-inducible kinase function in vivo. ACS Chem. Biol. 11(8), 2105-2111 (2016).

    2. Tarumoto, Y., Lin, S., Wang, J., et al. Salt-inducible kinase inhibition suppresses acute myeloid leukemia progression in vivo. Blood 135(1), 56-70 (2020).

    3. Wein, M.N., Liang, Y., Goransson, O., et al. SIKs control osteocyte responses to parathyroid hormone. Nat. Commun. 7, 13176 (2016).