kb NB 142-70

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kb NB 142-70 | CAS No. 1233533-04-4 | Protein Kinase D Inhibitors
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Description: Selective PKD inhibitor; analog of CID 755673 (Cat. No. 3327)

Chemical Name: 9-Hydroxy-3,4-dihydro-2H-[1]-benzothiolo[2,3-f][1,4]thiazepin-5-one

Purity: ≥98%

Product Details
Citations (4)
Supplemental Products
Reviews

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

M.Wt:
251.32
Formula:
C11H9NO2S2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at RT
CAS No:
1233533-04-4

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

  1. 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.
  2. 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):.
  3. 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):.
  4. PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors.
    Ni et al.
    PLoS ONE, 2013;9:e73149
  5. Novel protein kinase D inhibitors cause potent arrest in cancer cell growth and motility.
    LaValle et al.
    BMC Chemical Biology, 2010;10:5
  6. Synthesis and structure-activity relationships of benzothienothiazepinone inhibitors of protein kinase D.
    Bravo-Altamirano et al.
    ACS Med.Chem.Lett., 2011;2:154

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Citations for kb NB 142-70

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4 Citations: Showing 1 - 4

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