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1610536-69-0

中文名稱(chēng) 1610536-69-0
英文名稱(chēng) MELK-T1(JNJ-47117096) HCl
CAS 1610536-69-0
分子式 C21H23ClN4O2
分子量 398.89
MOL 文件 1610536-69-0.mol
更新日期 2024/11/11 16:08:01
1610536-69-0 結(jié)構(gòu)式 1610536-69-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11725
英文別名
MELK-T1 HCl
MELK-T1 HYDROCHLORIDE
MELK-T1(JNJ-47117096) HCl
JNJ-47117096 hydrochloride

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : ≥ 250 mg/mL (626.74 mM)
形態(tài)Solid
顏色White to off-white

常見(jiàn)問(wèn)題列表

生物活性
JNJ-47117096 hydrochloride 是一種有效的,選擇性的 MELK 抑制劑,IC50 值為 23 nM;同時(shí)對(duì) Flt3 的作用較強(qiáng),IC50 值為 18 nM。
靶點(diǎn)

IC50: 23 nM (MELK), 18 nM (Flt3)

體外研究

JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC 50 of 23 nM, also effectively inhibits Flt3, with an IC 50 of 18 nM, and slighitly blocks CAMKIIδ, Mnk2, CAMKIIγ, and MLCK (IC 50 , 810 nM, 760 nM, 1000 nM, 1000 nM). JNJ-47117096 (MELK-T1) suppresses the proliferation of Flt3-driven Ba/F3 cell lines, with an IC 50 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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