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JNJ-47117096 hydrochloride(MELK-T1 hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-47117096 hydrochloride(MELK-T1 hydrochloride)图片
CAS NO:1610536-69-0
规格:98%
分子量:398.89
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
JNJ-47117096hydrochloride是一种有效的,选择性的MELK抑制剂,IC50值为23nM;同时对Flt3的作用较强,IC50值为18nM。
CAS:1610536-69-0
分子式:C21H23ClN4O2
分子量:398.89
纯度:98%
存储:Store at -20°C

Background:

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.


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[1]. 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[2].



[1]. Johnson CN, et al. Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase. ACS Med Chem Lett. 2014 May 23;6(1):25-30. [2]. Beke L, et al. MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells. Biosci Rep. 2015 Oct 2;35(6). pii: e00267.