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    JNJ-47117096 HCl
    JNJ-47117096 HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4508
    CAS #: 1610536-69-0Purity ≥98%

    Description: JNJ-47117096 HCl (also known as MELK-T1), identified from a fragment-based drug design, is a novel, potent and selective MELK (maternal embryonic leucine zipper kinase) inhibitor with an IC50 of 23 nM, it also effectively inhibits Flt3, with an IC50 of 18 nM. Maternal embryonic leucine zipper kinase (MELK), a serine/threonine protein kinase, has oncogenic properties and is overexpressed in many cancer cells. The oncogenic function of MELK is attributed to its capacity to disable critical cell-cycle checkpoints and reduce replication stress.  MELK-T1 triggered a rapid and proteasome-dependent degradation of the MELK protein. Treatment of MCF-7 (Michigan Cancer Foundation-7) breast adenocarcinoma cells with MELK-T1 induced the accumulation of stalled replication forks and double-strand breaks that culminated in a replicative senescence phenotype. This phenotype correlated with a rapid and long-lasting ataxia telangiectasia-mutated (ATM) activation and phosphorylation of checkpoint kinase 2 (CHK2). Furthermore, MELK-T1 induced a strong phosphorylation of p53 (cellular tumour antigen p53), a prolonged up-regulation of p21 (cyclin-dependent kinase inhibitor 1) and a down-regulation of FOXM1 (Forkhead Box M1) target genes. Our data indicate that MELK is a key stimulator of proliferation by its ability to increase the threshold for DNA-damage tolerance (DDT). Thus, targeting MELK by the inhibition of both its catalytic activity and its protein stability might sensitize tumours to DNA-damaging agents or radiation therapy by lowering the DNA-damage threshold.

    References: ACS Med Chem Lett. 2014 May 23;6(1):25-30.Biosci Rep. 2015 Oct 2;35(6). pii: e00267.


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    JNJ-47117096 HCl

    Molecular Weight: 398.89
    Formula: C₂₁H₂₃ClN₄O₂
    CAS No.: 1610536-69-0
    SMILES: O=C(NC1=CC=C2CCNCCC2=C1)C3=CC=C(C4=CNN=C4)C=C3OC.Cl
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationJNJ-47117096 hydrochloride; JNJ 47117096 hydrochloride; JNJ47117096 hydrochloride; JNJ-47117096; JNJ-47117096 HCl; MELK T1; MELK-T1 HCl; MELK-T1


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    JNJ-47117096 HCl


    Inhibition of MELK by MELK-T1 (JNJ-47117096).  2015 Oct 2;35(6). pii: e00267.

     JNJ-47117096 HCl


    MELK-T1 triggers the proteasome-mediated degradation of MELK protein.

    JNJ-47117096 HCl

    MELK-T1 induces a delay in the progression of MCF-7 cells through S-phase.  2015 Oct 2;35(6). pii: e00267.

     JNJ-47117096 HCl


    Effects of MELK-T1 on DNA structure and replication.

    JNJ-47117096 HCl

    Model of how MELK increases the DDT barrier.  2015 Oct 2;35(6). pii: e00267.


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