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JNJ-47117096 hydrochloride

Catalog No. T11725 CAS 1610536-69-0

Synonyms: MELK-T1 hydrochloride

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.

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JNJ-47117096 hydrochloride Chemical Structure

JNJ-47117096 hydrochloride, CAS 1610536-69-0

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 766.00
50 mg	6-8 weeks	$ 996.00
100 mg	6-8 weeks	$ 1,740.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	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.
Targets&IC50	MELK:23 nM , FLT3:18 nM
In vitro	JNJ-47117096 demonstrates selectivity in its mechanism, showing no inhibitory effects on Ba/F3 cell proliferation transfected with FGFR1, FGFR3, or KDR, irrespective of IL-3 presence. At a concentration of 10 μM (MELK-T1), it notably slows MCF-7 cell progression through S-phase and targets MELK to induce replication forks stalling and DNA double-strand breaks (DSBs), subsequently activating the ATM-mediated DNA damage response (DDR). Furthermore, at 3 and 10 μM, it initiates growth arrest and a senescence phenotype, significantly increasing p53 phosphorylation, sustained p21 up-regulation, and down-regulation of FOXM1 target genes. As a MELK inhibitor, JNJ-47117096 hydrochloride exhibits potent and selective inhibition with an IC50 of 23 nM, also effectively inhibiting Flt3 (IC50 of 18 nM) and moderately affecting CAMKIIδ, Mnk2, CAMKIIγ, and MLCK (IC50s: 810 nM, 760 nM, 1000 nM, 1000 nM). Specifically, JNJ-47117096 (MELK-T1) suppresses Flt3-driven Ba/F3 cell line proliferation with an IC50 of 1.5 μM in the absence of IL-3, showing no inhibitory activity when IL-3 is present.

Synonyms	MELK-T1 hydrochloride
Molecular Weight	398.89
Formula	C21H23ClN4O2
CAS No.	1610536-69-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (626.74 mM)

References and Literature

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

JNJ-47117096 hydrochloride 1610536-69-0 Others JNJ 47117096 hydrochloride JNJ47117096 hydrochloride JNJ-47117096 Hydrochloride JNJ 47117096 Hydrochloride MELK-T1 hydrochloride JNJ47117096 Hydrochloride MELK-T1 Hydrochloride inhibitor inhibit

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