JNJ-47117096

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JNJ-47117096 is potent and selective MELK inhibitor, with an IC₅₀ of 23 nM, also effectively inhibits Flt3, with an IC₅₀ of 18 nM.

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JNJ-47117096 Chemical Structure

CAS No. : 1610586-62-3

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JNJ-47117096 hydrochloride

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Description	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].
IC₅₀ & Target	IC50: 23 nM (MELK), 18 nM (Flt3)^[1]
In Vitro	JNJ-47117096 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. JNJ-47117096 Related Antibodies
Molecular Weight	362.43
Formula	C₂₁H₂₂N₄O₂
CAS No.	1610586-62-3
SMILES	O=C(NC1=CC=C(CCNCC2)C2=C1)C3=CC=C(C4=CNN=C4)C=C3OC
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (273 KB) Handling Instructions (2659 KB)
References	[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. [Content Brief] [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. [Content Brief]

Kinase Assay ^[1]	Inhibition of MELK kinase activity is measured using a radioactive filter binding assay. Briefly, each assay well contains 1.25 nM MELK (human, residues 1-340) 10 μM ATP, 6.7 uCi/mL γ³³P-ATP, 3 μM biotinylated ZIP-tide peptide (Biotin-KKLNRTLSFAEPG) in 30 μL reaction buffer (25 mM Tris pH 7.5, 10 mM MgCl₂, 1 mM DTT, 1 mM EGTA, 0.1% Triton X100). Kinase reactions are performed for 25 minutes at room temperature before stopping with 40 μL 2% orthophosphoric acid. Unbound radioactivity is removed by filtering the reaction through a MAPH filter plate. The trapped ³³P labelled peptide is then washed twice with 200 μL 0.5% orthophosphoric acid, 20 μL Microscint-20 added per well and the amount of radioactivity determined by scintillation counting using a Topcount. To calculate compound IC₅₀, semi-log serial dilutions are used to produce 8-point dose-response curves in duplicate. IC₅₀ values are then derived using the four parameter logistic fit method in GraphPad Prism 5.0^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Compounds (JNJ-47117096) dissolved in DMSO are sprayed into 384-well plates (100 nL/well). A suspension of Ba/F3-Flt3 cells is added (20,000 cell/well), followed by the addition of 10 ng/mL IL3. The cells are incubated for 24 h at 37°C and 5% CO₂. Alamar Blue solution is added, and after 4 h incubation at 37°C, the fluorescent intensity is measured on a Fluorescence plate reader (540 nm excitation and 590 nm emission). The control experiment in the absence of IL3 is performed in the same way. To calculate compound IC₅₀, semi-log serial dilutions are used to produce 8- point dose-response curves in duplicate. A best-fit curve is fitted by a minimum sum of squares method to the plot of %Control vs. compound concentration. From this an IC₅₀ value is calculated^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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. [Content Brief] [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. [Content Brief]

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-471170961610586-62-3JNJ47117096JNJ 47117096MELKFLT3Maternal embryonic leucine zipper kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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JNJ-47117096

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