| Bioactivity | JNJ-47117096 is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM[1]. |
| Target | IC50: 23 nM (MELK), 18 nM (Flt3) |
| Invitro | JNJ-47117096 是一种强效且选择性的 MELK 抑制剂，IC50 为 23 nM，还可有效抑制 Flt3，IC50 为 18 nM，并轻微阻断 CAMKIIδ、Mnk2、CAMKIIγ 和 MLCK（IC50、810 nM、760 nM、1000 nM、1000 nM）。JNJ-47117096 (MELK-T1) 抑制 Flt3 驱动的 Ba/F3 细胞系的增殖，在没有 IL-3 的情况下 IC50 为 1.5 μM，而在有 IL-3 的情况下未观察到抑制活性。JNJ-47117096 不会抑制转染了 FGFR1、FGFR3 或 KDR 的 Ba/F3 细胞系的增殖，无论有无 IL-3[1]。JNJ-47117096 (MELK-T1, 10 μM) 会延迟 MCF-7 细胞进入 S 期。JNJ-47117096 抑制 MELK，然后发挥停滞的复制叉和 DNA 双链断裂 (DSB)。 JNJ-47117096 可激活 ATM 介导的 DNA 损伤反应 (DDR)。JNJ-47117096 (3, 10 μM) 可导致生长停滞和衰老表型。此外，JNJ-47117096 可诱导 p53 的强烈磷酸化、p21 的长期上调和 FOXM1 靶基因的下调[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> JNJ-47117096 相关抗体: |
| CAS | 1610586-62-3 |
| Formula | C21H22N4O2 |
| Molar Mass | 362.43 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
JNJ-47117096
CAS: 1610586-62-3 F: C21H22N4O2 W: 362.43
JNJ-47117096 is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50
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