A MELK inhibitor
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JNJ-47117096 (trifluoroacetate salt)

Item No. 41605

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methoxy-4-(1H-pyrazol-4-yl)-N-(2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)-benzamide, trifluoroacetate salt
Molecular Formula
C21H22N4O2 • CF3COOH
Formula Weight
476.4
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C1=CC=C(C2=CNN=C2)C=C1OC)NC3=CC=C4C(CCNCC4)=C3.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C21H22N4O2.C2HF3O2/c1-27-20-11-15(17-12-23-24-13-17)3-5-19(20)21(26)25-18-4-2-14-6-8-22-9-7-16(14)10-18;3-2(4,5)1(6)7/h2-5,10-13,22H,6-9H2,1H3,(H,23,24)(H,25,26);(H,6,7)
InChi Key
DBSZBFCNMCPGCJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $53

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    5 mg

    $238

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    10 mg

    $423

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    25 mg

    $924

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    Product Description

    JNJ-47117096 is an inhibitor of maternal embryonic leucine zipper kinase (MELK; IC50 = 37 nM).1 It is selective for MELK over calcium/calmodulin-dependent protein kinase δ (CAMKIIδ), MAP kinase-interacting serine/threonine protein kinase 2 (MNK2), CAMKIIγ, and myosin light-chain kinase (MLCK; IC50s = 810, 760, 1,000, and 1,000 nM, respectively) but does inhibit FMS-related tyrosine kinase 3 (FLT3; IC50 = 18 nM). JNJ-47117096 inhibits autophosphorylation of MELK (IC50 = 0.52 µM) and proteasome-dependent degradation of MELK in MCF-7 cells.2 It induces cellular senescence and the DNA damage response mediated by ataxia-telangiectasia and Rad3-related protein kinase (ATM) in MCF-7 cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Johnson, C.N., Berdini, V., Beke, L., et al. Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase. ACS Med. Chem. Lett. 6(1), 25-30 (2014).

    2. Beke, L., Kig, C., Linders, J.T., et al. MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells. Biosci. Rep. 35(6), e00267 (2015).