2. PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK
  3. MELK FLT3
  4. JNJ-47117096 hydrochloride

JNJ-47117096 hydrochloride  (Synonyms: MELK-T1 hydrochloride)

目录号: HY-12420 纯度: 99.68%
COA 产品使用指南

摩尔计算器

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。

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JNJ-47117096 hydrochloride Chemical Structure

JNJ-47117096 hydrochloride Chemical Structure

CAS No. : 1610536-69-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2600
In-stock
1 mg ￥1045
In-stock
5 mg ￥2300
In-stock
10 mg ￥3900
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

JNJ-47117096 hydrochloride 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target

IC50: 23 nM (MELK), 18 nM (Flt3)[1]
体外研究
(In Vitro)

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-47117096 hydrochloride 相关抗体:
分子量

398.89

Formula

C21H23ClN4O2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 250 mg/mL (626.74 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : 3.33 mg/mL (8.35 mM; 超声助溶 (<60°C))

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5070 mL 12.5348 mL 25.0696 mL
5 mM 0.5014 mL 2.5070 mL 5.0139 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
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.
参考文献

JNJ-47117096 hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.5070 mL 12.5348 mL 25.0696 mL 62.6739 mL
5 mM 0.5014 mL 2.5070 mL 5.0139 mL 12.5348 mL
DMSO 10 mM 0.2507 mL 1.2535 mL 2.5070 mL 6.2674 mL
15 mM 0.1671 mL 0.8357 mL 1.6713 mL 4.1783 mL
20 mM 0.1253 mL 0.6267 mL 1.2535 mL 3.1337 mL
25 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.5070 mL
30 mM 0.0836 mL 0.4178 mL 0.8357 mL 2.0891 mL
40 mM 0.0627 mL 0.3134 mL 0.6267 mL 1.5668 mL
50 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2535 mL
60 mM 0.0418 mL 0.2089 mL 0.4178 mL 1.0446 mL
80 mM 0.0313 mL 0.1567 mL 0.3134 mL 0.7834 mL
100 mM 0.0251 mL 0.1253 mL 0.2507 mL 0.6267 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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-471170961610536-69-0MELK-T1JNJ47117096JNJ 47117096MELKFLT3Maternal embryonic leucine zipper kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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