A SIK inhibitor
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YKL-06-061

Item No. 41721

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlChloroform: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $83

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    10 mg

    $158

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    25 mg

    $248

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    50 mg

    $372

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    Product Description

    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).1 It is selective for these SIKs over a panel of 468 additional kinases at 1 µM but does inhibit FRK, CSF1R, p38α, p38β, 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, PDGFRβ, 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; Item No. 18682).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mujahid, N., Liang, Y., Murakami, R., et al. A UV-independent topical small-molecule approach for melanin production in human skin. Cell Rep. 19(11), 2177-2184 (2017).

    2. Peng, L., Li, C., Tang, X., et al. Blocking salt-inducible kinases with YKL-06-061 prevents PTZ-induced seizures in mice. Brain Behav. 13(12), e3305 (2023).