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。

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.

Solid

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

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 respon

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : ≥ 250 mg/mL (626.74 mM)H₂O : 3.33 mg/mL (8.35 mM; ultrasonic and warming and heat to 60°C)