HTH-01-015

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

HTH-01-015  纯度: 99.18%

HTH-01-015 是一种选择性 NUAK1/ARK5 抑制剂 (IC50 为 100 nM)。HTH-01-015 抑制 NUAK1 的效力比抑制 NUAK2 高 100 倍以上 (IC50>10 μM)。

HTH-01-015

HTH-01-015 Chemical Structure

CAS No. : 1613724-42-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥880 In-stock
5 mg ¥800 In-stock
10 mg ¥1200 In-stock
50 mg ¥3600 In-stock
100 mg ¥4850 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

HTH-01-015 is a selective NUAK1/ARK5 inhibitor (IC50 is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).

IC50 & Target[1]

NUAK1

100 nM (IC50)

体外研究
(In Vitro)

HTH-01-015 is a specific NUAK1 inhibitor. The related NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumor suppressor kinase. HTH-01-015 inhibits NUAK1 with an IC50 of 100 nM, but does not significantly inhibit NUAK2 (IC50 of >10 μM). In all cell lines tested, HTH-01-015 inhibits the phosphorylation of the only well-characterized substrate, MYPT1 (myosin phosphate-targeting subunit 1) that is phosphorylated by NUAK1 at Ser445. In U2OS cells, HTH-01-015 suppresses proliferation and phosphorylation of MYPT1 to the same extent as shRNA-mediated NUAK1 knockdown. In mouse embryonic fibroblasts (MEFs), treatment with 10 μM HTH-01-015 suppresses proliferation and phosphorylation of MYPT1 to the same extent as NUAK1-knockout. To test whether NUAK1 inhibition impaired the ability of the invasive U2OS cells to enter a matrix, 3D Matrigel Transwell invasion assays demonstrate that 10 μM HTH-01-015 markedly inhibits the invasiveness of U2OS cells in this assay[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

468.55

Formula

C26H28N8O

CAS 号

1613724-42-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (213.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1342 mL 10.6712 mL 21.3424 mL
5 mM 0.4268 mL 2.1342 mL 4.2685 mL
10 mM 0.2134 mL 1.0671 mL 2.1342 mL

*

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.34 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.34 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.34 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Banerjee S, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25.

Kinase Assay
[1]

Kinase inhibitor specificity profiling assays are carried out against a panel of 140 protein kinases. Results are presented as a percentage of kinase activity in DMSO control reactions. Protein kinases are assayed in vitro with 0.1 or 1 μM of the inhibitors (e.g., HTH-01-015) and the results are presented as an average of triplicate reactions±S.D. or in the form of comparative histograms[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay kit. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM HTH-01-015 or WZ4003. The ability of U2OS cells to invade in the presence or absence of 10 μM HTH-01-015 or WZ4003 is tested in a growth-factor-reduced Matrigel invasion chamber. Cells are serum-deprived for 2 h, detached using cell-dissociation buffer, and 2.5×105 cells suspended in DMEM containing 1% (w/v) BSA are added to the upper chambers in triplicate and chemoattractant [DMEM containing 10% (v/v) FBS] is added to the lower wells. The chambers are kept at 37°C in 5% CO2 for 16 h in the presence or absence of 10 μM HTH-01-015 or WZ4003 both in the upper and lower wells. Non-invaded cells are removed from the upper face of the filters by scraping, and cells that have migrated to the lower face of the filters are fixed and stained with Reastain Quick-Diff kit and images (×10 magnification) are captured. For cell invasion assays, statistical significance is assessed using GraphPad Prism 5.0[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Banerjee S, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25.

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