kb NB 142-70

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。

kb NB 142-70  纯度: 98.85%

kb NB 142-70 是一种有效的 PKD 抑制剂,对 PKD1,PKD2 和 PKD3 的 IC50 值分别为 28.3 nM,58.7 nM 和 53.2 nM;kb NB 142-70 同时具有抗肿瘤活性。

kb NB 142-70

kb NB 142-70 Chemical Structure

CAS No. : 1233533-04-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1595 In-stock
10 mg ¥1450 In-stock
50 mg ¥6450 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

kb NB 142-70 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library

生物活性

kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.

IC50 & Target[1]

PKD1

28.3 nM (IC50)

PKD3

53.2 nM (IC50)

PKD2

58.7 nM (IC50)

体外研究
(In Vitro)

kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also inhibits Ser916 phosphorylation of PKD1 (IC50, 2.2 ± 0.6 μM) in LNCaP cells. Moreover, kb NB 142-70 is cytotoxic against PC3 cells with an EC50 of 8.025 μM[1]. kb NB 142-70 (0-5 μM) concentration-dependently prevents ANG II-induced phosphorylation of HDAC4 at Ser246 and Ser632, HDAC5 at Ser259 and Ser498, and HDAC7 at Ser155 in IEC-18 cells. In addition, kb NB 142-70 (3.5 μM) also suppresses HDAC4, HDAC5, and HDAC7 phosphorylation in IEC-18 cells stimulated with ANG II for 0-240 min or with vasopressin, lysophosphatidic acid (LPA), or phorbol 12,13-dibutyrate (PDBu)[2].

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

251.32

Formula

C11H9NO2S2

CAS 号

1233533-04-4

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 : 46.67 mg/mL (185.70 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9790 mL 19.8950 mL 39.7899 mL
5 mM 0.7958 mL 3.9790 mL 7.9580 mL
10 mM 0.3979 mL 1.9895 mL 3.9790 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3.5 mg/mL (13.93 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (13.93 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 35.0 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
  • 2.

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

    Solubility: ≥ 3.5 mg/mL (13.93 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (13.93 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 35.0 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]. Lavalle CR, et al. Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility. BMC Chem Biol. 2010 May 5;10:5.

    [2]. James Sinnett-Smith, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol. 2014 May 15; 306(10): C961-C971.

Cell Assay
[1]

Briefly, PC3 cells are treated with kb NB 142-70 at 10 μM concentration for 48 h, and then fixed in 70% ice-cold ethanol overnight and labeled with propidium iodide. The labeled cells are analyzed using a FACScan Benchtop Cytometer[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]. Lavalle CR, et al. Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility. BMC Chem Biol. 2010 May 5;10:5.

    [2]. James Sinnett-Smith, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol. 2014 May 15; 306(10): C961-C971.

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