An inhibitor of RSKs
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LJI308

Item No. 19924

Technical Information
Formal Name
2,6-difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]-phenol
CAS Number
1627709-94-7
Molecular Formula
C21H18F2N2O2
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml
λmax
317 nm
SMILES
FC1=CC(C2=CN=CC=C2C3=CC=C(N4CCOCC4)C=C3)=CC(F)=C1O
InChi Code
InChI=1S/C21H18F2N2O2/c22-19-11-15(12-20(23)21(19)26)18-13-24-6-5-17(18)14-1-3-16(4-2-14)25-7-9-27-10-8-25/h1-6,11-13,26H,7-10H2
InChi Key
YUYJEQHNWKQNBT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LJI308 is a selective and potent inhibitor of the p90 ribosomal S6 kinase (RSK) family with IC50 values ranging from 4 to 13 nM for RSK isoforms 1-3.1,2 In a panel of 442 kinases, LJI308 is selective for RSK1, RSK3, and RSK4. It also inhibits S6K1, MEK4, and HIP in the low micromolar range but had no effect on other kinases tested.1 LJI308 also reduces phosphorylation of Y-box-binding protein (YB1) in MDA-MB-231 cells bearing activating mutations in the MAPK signaling pathway (EC50 = 0.21 μM) and reduces H358 growth in soft agar and colony forming assays.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Aronchik, I., Appleton, B.A., Basham, S.E., et alNovel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol. Cancer Res. 12(5), 803-812 (2014).

    2. Jain, R., Mathur, M., Lan, J., et alDiscovery of potent and selective RSK inhibitors as biological probes. J. Med. Chem. 58(17), 6766-6783 (2015).