kb NB 142-70

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Cat.No. 3962 - kb NB 142-70 | C11H9NO2S2 | CAS No. 1233533-04-4
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)
Datasheet
Citations (3)
Reviews
Literature

Biological Activity

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
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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25.13 100

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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References

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


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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

3 Citations for kb NB 142-70

Citations are publications that use Tocris products. Selected citations for kb NB 142-70 include:

Zhang et al (2017) Protein kinase D at the Golgi controls NLRP3 inflammasome activation. J Exp Med 214 2671 PMID: 28716882

Xiong et al (2016) Protein Kinase D2 Protects against Acute Colitis Induced by Dextran Sulfate Sodium in Mice. Sci Rep 6 34079 PMID: 27659202

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


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Literature in this Area

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Cancer

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