CAS 1233533-04-4|kb-NB142-70
| Common Name | kb-NB142-70 | ||
|---|---|---|---|
| CAS Number | 1233533-04-4 | Molecular Weight | 251.325 |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 601.9±55.0 °C at 760 mmHg |
| Molecular Formula | C11H9NO2S2 | Melting Point | / |
| MSDS | USA | Flash Point | 317.8±31.5 °C |
Names
| Name | 3,4-Dihydro-9-hydroxy-[1]benzothieno[2,3-f]-1,4-thiazepin-5(2H)-one |
|---|---|
| Synonym | More Synonyms |
kb-NB142-70 BiologicalActivity
| Description | 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 has antitumor activity. |
|---|---|
| Related Catalog | Signaling Pathways >>Apoptosis >>PKDResearch Areas >>Cancer |
| Target | PKD1:28.3 nM (IC50) PKD3:53.2 nM (IC50) PKD2:58.7 nM (IC50) |
| 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 Ser916 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[1]. kb NB 142-70 (0-5 μM) concentration-dependently prevents ANG II-induced phosphorylation of HDAC4 at Ser246 and Ser632, HDAC5 at Ser259 and Ser498, and HDAC7 at Ser155 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)[2]. |
| Cell Assay | Briefly, PC3 cells are treated with kb NB 142-70 at 10 μM concentration for 48 h, and then fixed in 70% ice-cold ethanol overnight and labeled with propidium iodide. The labeled cells are analyzed using a FACScan Benchtop Cytometer[1]. |
| References | [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. |
Chemical & Physical Properties
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 601.9±55.0 °C at 760 mmHg |
| Molecular Formula | C11H9NO2S2 |
| Molecular Weight | 251.325 |
| Flash Point | 317.8±31.5 °C |
| Exact Mass | 251.007462 |
| PSA | 106.36000 |
| LogP | 2.39 |
| Appearance of Characters | white solid |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.746 |
| InChIKey | DHUAGGSHTKPOHU-UHFFFAOYSA-N |
| SMILES | O=C1NCCSc2c1sc1ccc(O)cc21 |
| Storage condition | -20℃ |
Safety Information
| RIDADR | NONH for all modes of transport |
|---|
Articles3
More Articles| Targeting vascular endothelial growth factor receptor 2 and protein kinase D1 related pathways by a multiple kinase inhibitor in angiogenesis and inflammation related processes in vitro. PLoS ONE 10(4) , e0124234, (2015) Emerging evidence suggests that the vascular endothelial growth factor receptor 2 (VEGFR2) and protein kinase D1 (PKD1) signaling axis plays a critical role in normal and pathological angiogenesis and... | |
| PKD1 is downregulated in non-small cell lung cancer and mediates the feedback inhibition of mTORC1-S6K1 axis in response to phorbol ester. Int. J. Biochem. Cell Biol. 60 , 34-42, (2015) Protein kinase D1 (PKD1) is increasingly implicated in multiple biological and molecular events that regulate the proliferation or invasiveness in several cancers. However, little is known about the e... | |
| Positive cross talk between protein kinase D and β-catenin in intestinal epithelial cells: impact on β-catenin nuclear localization and phosphorylation at Ser552. Am. J. Physiol. Cell Physiol. 310 , C542-57, (2016) Given the fundamental role of β-catenin signaling in intestinal epithelial cell proliferation and the growth-promoting function of protein kinase D1 (PKD1) in these cells, we hypothesized that PKDs me... |
Synonyms
| [1]Benzothieno[2,3-f]-1,4-thiazepin-5(2H)-one, 3,4-dihydro-9-hydroxy- |
| 9-Hydroxy-3,4-dihydro[1]benzothieno[2,3-f][1,4]thiazepin-5(2H)-one |
| 9-hydroxy-3,4-dihydro-2H-[1]benzothiolo[2,3-f][1,4]thiazepin-5-one |
| kb NB 142-70 |
