kb NB 142-70

A selective PKD inhibitor

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10mg

￥1287.00

1030.00

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50mg

￥5150.00

4120.00

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货号: ajci6880
CAS: 1233533-04-4
别名: 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
分子式: C11H9NO2S2
分子量: 251.32
纯度: >98%
溶解度: ≥ 12.9 mg/mL in DMSO, ≥ 8.05 mg/mL in EtOH with ultrasonic and warming
储存: Store at -20°C
库存: 现货

Background

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.

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].

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.

Protocol

Cell experiment:

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].

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.