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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% (HPLC)
Biological Activity for kb NB 142-70
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 for kb NB 142-70
| M. Wt | 251.32 |
| Formula | C11H9NO2S2 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1233533-04-4 |
| PubChem ID | 45258277 |
| InChI Key | DHUAGGSHTKPOHU-UHFFFAOYSA-N |
| Smiles | OC1=CC=C(SC3=C2SCCNC3=O)C2=C1 |
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.
Solubility Data for kb NB 142-70
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.13 | 100 |
Preparing Stock Solutions for kb NB 142-70
The following data is based on the product molecular weight 251.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.98 mL | 19.89 mL | 39.79 mL |
| 5 mM | 0.8 mL | 3.98 mL | 7.96 mL |
| 10 mM | 0.4 mL | 1.99 mL | 3.98 mL |
| 50 mM | 0.08 mL | 0.4 mL | 0.8 mL |
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Product Datasheets for kb NB 142-70
References for kb NB 142-70
References are publications that support the biological activity of the product.
LaValle et al (2010) Novel protein kinase D inhibitors cause potent arrest in cancer cell growth and motility. BMC Chemical Biology 10 5 PMID: 20444281
Bravo-Altamirano et al (2011) Synthesis and structure-activity relationships of benzothienothiazepinone inhibitors of protein kinase D. ACS Med.Chem.Lett. 2 154 PMID: 21617763
Ni et al (2013) PKD1 mediates negative feedback of PI3K/Akt activation in response to G protein-coupled receptors. PLoS One 8 e73149 PMID: 24039875
If you know of a relevant reference for kb NB 142-70, please let us know.
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Keywords: kb NB 142-70, kb NB 142-70 supplier, PKD, protein, kinase, D, inhibitor, analog, selective, inhibitors, inhibits, analogs, kbNB142-70, Protein, Kinase, 3962, Tocris Bioscience
4 Citations for kb NB 142-70
Citations are publications that use Tocris products. Selected citations for kb NB 142-70 include:
Stephan A et al (2021) Protein kinase D promotes activity-dependent AMPA receptor endocytosis in hippocampal neurons. Traffic 22 454-470 PMID: 34564930
Weber et al (2015) A computational model of PKD and CERT interactions at the trans-Golgi network of mammalian cells. BMC Syst Biol 9 9 PMID: 25889812
Xiong et al (2016) Protein Kinase D2 Protects against Acute Colitis Induced by Dextran Sulfate Sodium in Mice. Sci Rep 6 34079 PMID: 27659202
Zhang et al (2017) Protein kinase D at the Golgi controls NLRP3 inflammasome activation. J Exp Med 214 2671 PMID: 28716882
Do you know of a great paper that uses kb NB 142-70 from Tocris? Please let us know.
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