kb NB 142-70
Chemical Name: 9-Hydroxy-3,4-dihydro-2H-[1]-benzothiolo[2,3-f][1,4]thiazepin-5-one
Purity: ≥98%
Biological Activity
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively). More potent analog of CID 755673 (Cat. No. 3327) with 7-fold greater inhibition. Inhibits prostrate cancer cell migration and invasion and reduces wound healing in vitro; displays prominent cytotoxic and anti-proliferative effects.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
-
Protein kinase D promotes airway epithelial barrier dysfunction and permeability through down-regulation of claudin-1.
Gan H, Wang G, Hao Q, Wang Q, Tang H
J Biol Chem, 2014;288(52):37343-54. -
Protein kinase D1 (PKD1) phosphorylation on Ser(203) by type I p21-activated kinase (PAK) regulates PKD1 localization
JK Chang, Y Ni, L Han, J Sinnett-Sm, R Jacamo, O Rey, SH Young, E Rozengurt
J. Biol. Chem., 2017;0(0):. -
Insulin Receptor and GPCR Crosstalk Stimulates YAP via PI3K and PKD in Pancreatic Cancer Cells
F Hao, Q Xu, Y Zhao, JV Stevens, SH Young, J Sinnett-Sm, E Rozengurt
Mol. Cancer Res., 2017;0(0):. -
PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors.
Ni et al.
PLoS ONE, 2013;9:e73149 -
Novel protein kinase D inhibitors cause potent arrest in cancer cell growth and motility.
LaValle et al.
BMC Chemical Biology, 2010;10:5 -
Synthesis and structure-activity relationships of benzothienothiazepinone inhibitors of protein kinase D.
Bravo-Altamirano et al.
ACS Med.Chem.Lett., 2011;2:154
Product Datasheets
Reconstitution Calculator
Molarity Calculator
Citations for kb NB 142-70
The citations listed below are publications that use Tocris products. Selected citations for kb NB 142-70 include:
4 Citations: Showing 1 - 4
-
Protein kinase D promotes activity-dependent AMPA receptor endocytosis in hippocampal neurons.
Authors: Stephan A Et al.
Traffic 2021;22:454-470
-
Protein kinase D at the Golgi controls NLRP3 inflammasome activation.
Authors: Zhang Et al.
J Exp Med 2017;214:2671
-
Protein Kinase D2 Protects against Acute Colitis Induced by Dextran Sulfate Sodium in Mice.
Authors: Xiong Et al.
Sci Rep 2016;6:34079
-
A computational model of PKD and CERT interactions at the trans-Golgi network of mammalian cells.
Authors: Weber Et al.
BMC Syst Biol 2015;9:9
FAQs
No product specific FAQs exist for this product, however you may
View all Small Molecule FAQsReviews for kb NB 142-70
There are currently no reviews for this product. Be the first to review kb NB 142-70 and earn rewards!
Have you used kb NB 142-70?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image