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kb NB 142-70 Sale

(Synonyms: 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) 目录号 : GC11319

A selective PKD inhibitor

kb NB 142-70 Chemical Structure

Cas No.:1233533-04-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥431.00
现货
10mg
¥1,071.00
现货
50mg
¥4,305.00
现货

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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].

References:

[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.

产品描述

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].

References:
[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.

Chemical Properties

Cas No. 1233533-04-4 SDF
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
化学名 9-hydroxy-3,4-dihydro-2H-[1]benzothiolo[2,3-f][1,4]thiazepin-5-one
Canonical SMILES C1CSC2=C(C(=O)N1)SC3=C2C=C(C=C3)O
分子式 C11H9NO2S2 分子量 251.32
溶解度 ≥ 12.9 mg/mL in DMSO, ≥ 8.05 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
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1 mM 3.979 mL 19.895 mL 39.7899 mL
5 mM 0.7958 mL 3.979 mL 7.958 mL
10 mM 0.3979 mL 1.9895 mL 3.979 mL
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