An inhibitor of RSKs
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LJH685

Item No. 19913

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,6-difluoro-4-[4-[4-(4-methyl-1-piperazinyl)phenyl]-3-pyridinyl]-phenol
CAS Number
1627710-50-2
Molecular Formula
C22H21F2N3O
Formula Weight
381.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:7): 0.125 mg/mlEthanol: 2.5 mg/ml
λmax
237, 270, 316 nm
SMILES
CN(CC1)CCN1C(C=C2)=CC=C2C3=CC=NC=C3C4=CC(F)=C(O)C(F)=C4
InChi Code
InChI=1S/C22H21F2N3O/c1-26-8-10-27(11-9-26)17-4-2-15(3-5-17)18-6-7-25-14-19(18)16-12-20(23)22(28)21(24)13-16/h2-7,12-14,28H,8-11H2,1H3
InChi Key
IKUFKDGKRLMXEX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $236

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    25 mg

    $502

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    Product Description

    LJH685 is an inhibitor of p90 ribosomal S6 kinases (RSKs, also known as MAP kinase-activated protein kinases, or MAPKAPKs) that inhibits RSK1, 2, and 3 in vitro with IC50 values of 6, 5, and 4 nM, respectively.1 It is selective for RSKs over a panel of 96 other kinases. LJH685 blocks RSK activity in cells, preventing phosphorylation of y-box-binding protein 1 on Ser102.1 The inhibition of RSK activity correlates with antiproliferative effects in MAPK pathway-dependent cancer cell lines, but only in an anchorage-independent growth setting.1

    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 al. Novel 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).