3,4-二氢-9-羟基-[1]苯并噻吩并[2,3-f]-1,4-硫氮杂革-5(2H)-酮;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;kb NB 142-70
英文名称
kb NB 142-70
英文别名
kb-NB142-70;3,4-Dihydro-9-hydroxy-[1]benzothieno-[2,3-f]-1,4-thiazepin-5(2H)-one;3,4-Dihydro-9-hydroxy-[1]benzothieno[2,3-f]-1,4-thiazepin-5(2H)-one;kb NB 142-70;AG-L-65866;CHEBI:1169969;CHEMBL1672571;CS-1091;CTK8G0429;QCR-15;SureCN9920595;9-hydroxy-3,4-dihydro-2H-[1]benzothiolo[2,3-f][1,4]thiazepin-5-one;DHUAGGSHTKPOHU-UHFFFAOYSA-N;GTPL9369;AOB1401;SYN5189;HMS3740G15;BCP06729;BDBM50336960;3758AH;AB0094895;kb-
kb NB 142-70 is a potent PKD inhibitor, with IC 50 s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.
性状
Solid
IC50 & Target[1][2]
PKD1 28.3 nM (IC50) PKD3 53.2 nM (IC5
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 Ser 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. kb NB 142-70 (0-5 μM) concentration-dependently prevents ANG II-induced phosphorylation of HDAC4 at Ser and Ser, HDAC5 at Ser and Ser, and HDAC7 at Ser 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). has not independently confirmed the accuracy of these methods. They are for reference only.
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
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.
溶解度数据
In Vitro: DMSO : 46.67 mg/mL (185.70 mM; Need ultrasonic)配制储备液