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JNJ-47117096 hydrochloride

CAS No. : 1610536-69-0

MCE 国际站：JNJ-47117096 hydrochloride

产品活性：JNJ-47117096 hydrochloride 是一种有效的，选择性的 MELK 抑制剂，IC₅₀ 值为 23 nM；同时对 Flt3 的作用较强，IC₅₀ 值为 18 nM。

研究领域：PI3K/Akt/mTOR  |  Protein Tyrosine Kinase/RTK

作用靶点：MELK  |  FLT3

In Vitro: JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC₅₀ of 23 nM, also effectively inhibits Flt3, with an IC₅₀ of 18 nM, and slighitly blocks CAMKIIδ, Mnk2, CAMKIIγ, and MLCK (IC₅₀, 810 nM, 760 nM, 1000 nM, 1000 nM). JNJ-47117096 (MELK-T1) suppresses the proliferation of Flt3-driven Ba/F3 cell lines, with an IC₅₀ of 1.5 μM in the absence of IL-3, while no inhibitory activity is observed in the presence of IL-3. JNJ-47117096 does not inhibit the proliferation of Ba/F3 cell lines transfected with either FGFR1, FGFR3, or KDR, either in the presence or absence of IL-3. JNJ-47117096 (MELK-T1, 10 μM) delays the progression of MCF-7 cells through S-phase. JNJ-47117096 inhibits MELK, and then exerts stalled replication forks and DNA double-strand breaks (DSBs). JNJ-47117096 activates the ATM-mediated DNA-damage response (DDR). JNJ-47117096 (3, 10 μM) results in a growth arrest and a senescent phenotype. Moreover, JNJ-47117096 induces a strong phosphorylation of p53, a prolonged up-regulation of p21 and a down-regulation of FOXM1 target genes.

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