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3,4-二氢-9-羟基-[1]苯并噻吩并[2,3-F]-1,4-硫氮杂卓-5(2H)-酮

用途

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。

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名称

[ CAS 号 ]:
1233533-04-4

[ 中文名 ]:
3,4-二氢-9-羟基-[1]苯并噻吩并[2,3-F]-1,4-硫氮杂卓-5(2H)-酮

[ 英文名 ]:
kb-NB142-70

[英文别名 ]:

kb NB 142-70

生物活性

[ 描述 ]:

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。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> PKD

研究领域 >> 癌症

[ 靶点 ]

PKD1:28.3 nM (IC50)

PKD3:53.2 nM (IC50)

PKD2:58.7 nM (IC50)

[体外研究]

kb NB 142-70是一种有效的PKD抑制剂,PKD1,PKD2和PKD3的IC50分别为28.3,58.7和53.2 nM。 kb NB 142-70还抑制LNCaP细胞中PKD1的Ser916磷酸化(IC50,2.2±0.6μM)。此外,kb NB 142-70对PC3细胞具有细胞毒性,EC50为8.025μM[1]。 kb NB 142-70(0-5μM)浓度依赖性地阻止ANG II诱导的Ser246和Ser632处的HDAC4,Ser259和Ser498处的HDAC5以及IEC-18细胞中Ser155处的HDAC7的磷酸化。此外,kb NB 142-70(3.5μM)还抑制用ANG II刺激0-240分钟或用加压素,溶血磷脂酸(LPA)或佛波醇12,13刺激的IEC-18细胞中的HDAC4,HDAC5和HDAC7磷酸化。 -dibutyrate(PDBu)[2]。

[细胞实验]

简言之，将PC3细胞用10μM浓度的kb NB 142-70处理48小时，然后在70％冰冷的乙醇中固定过夜并用碘化丙锭标记。使用FACScan台式细胞仪[1]分析标记的细胞。

[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.

[相关活性小分子]

PP1模拟II,1NM-PP1 | 2,3,4,5-四氢-7-羟基-1H-苯并呋喃并[2,3-c]氮杂卓-1-酮 | CRT0066101二盐酸盐 | CID 2011756

物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
601.9±55.0 °C at 760 mmHg

[ 分子式 ]:
C₁₁H₉NO₂S₂

[ 分子量 ]:
251.325

[ 闪点 ]:
317.8±31.5 °C

[ 精确质量 ]:
251.007462

[ PSA ]:
106.36000

[ LogP ]:
2.39

[ 外观性状 ]:
white solid

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.746

[ 储存条件 ]:
-20℃

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

合成路线

详细合成路线

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文献

Targeting vascular endothelial growth factor receptor 2 and protein kinase D1 related pathways by a multiple kinase inhibitor in angiogenesis and inflammation related processes in vitro.

PLoS ONE 10(4) , e0124234, (2015)

Emerging evidence suggests that the vascular endothelial growth factor receptor 2 (VEGFR2) and protein kinase D1 (PKD1) signaling axis plays a critical role in normal and pathological angiogenesis and...

PKD1 is downregulated in non-small cell lung cancer and mediates the feedback inhibition of mTORC1-S6K1 axis in response to phorbol ester.

Int. J. Biochem. Cell Biol. 60 , 34-42, (2015)

Protein kinase D1 (PKD1) is increasingly implicated in multiple biological and molecular events that regulate the proliferation or invasiveness in several cancers. However, little is known about the e...

Positive cross talk between protein kinase D and β-catenin in intestinal epithelial cells: impact on β-catenin nuclear localization and phosphorylation at Ser552.

Am. J. Physiol. Cell Physiol. 310 , C542-57, (2016)

Given the fundamental role of β-catenin signaling in intestinal epithelial cell proliferation and the growth-promoting function of protein kinase D1 (PKD1) in these cells, we hypothesized that PKDs me...

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