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Submit ReviewCID 755673
Description: Selective protein kinase D inhibitor
Chemical Name: 2,3,4,5-Tetrahydro-7-hydroxy-1H-benzofuro[2,3-c]azepin-1-one
Purity: ≥98% (HPLC)
Biological Activity for CID 755673
CID 755673 is a selective protein kinase D (PKD) inhibitor (IC50 values are 0.182, 0.280, 0.227, >10, 15.3, 20.3, 40.5 and >50 μM at PKD1, PKD2, PKD3, PKC, CAK, PLK1, CAMKIIα and Akt respectively). Blocks PKD-mediated protein transport and inhibits prostate cancer cell proliferation, migration and invasion in vitro.
Compound Libraries for CID 755673
CID 755673 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for CID 755673
| M. Wt | 217.22 |
| Formula | C12H11NO3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 521937-07-5 |
| PubChem ID | 755673 |
| InChI Key | AACFPJSJOWQNBN-UHFFFAOYSA-N |
| Smiles | OC1=CC2=C(OC3=C2CCCNC3=O)C=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 CID 755673
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 21.72 | 100 |
Preparing Stock Solutions for CID 755673
The following data is based on the product molecular weight 217.22. 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 | 4.6 mL | 23.02 mL | 46.04 mL |
| 5 mM | 0.92 mL | 4.6 mL | 9.21 mL |
| 10 mM | 0.46 mL | 2.3 mL | 4.6 mL |
| 50 mM | 0.09 mL | 0.46 mL | 0.92 mL |
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Product Datasheets for CID 755673
References for CID 755673
References are publications that support the biological activity of the product.
Sharlow et al (2008) Potent and selective disruption of protein kinase D functionality by benzoxoloazepinolone. J.Biol.Chem. 283 33516 PMID: 18829454
If you know of a relevant reference for CID 755673, please let us know.
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Keywords: CID 755673, CID 755673 supplier, Selective, protein, kinases, D, inhibitors, inhibits, PKD, CID755673, Protein, Kinase, 3327, Tocris Bioscience
12 Citations for CID 755673
Citations are publications that use Tocris products. Selected citations for CID 755673 include:
Subathra et al (2011) Sphingomyelin synthases regulate protein trafficking and secretion. PLoS One 6 e23644 PMID: 21980337
Qureshi et al (2011) Role of sphingomyelin synthase in controlling the antimicrobial activity of neutrophils against Cryptococcus neoformans. PLoS One 5 e15587 PMID: 21203393
Bhattacharya et al (2011) Bcr-abl signals to desensitize chronic myeloid leukemia cells to IFNα via accelerating the degradation of its receptor. Blood 118 4179 PMID: 21821707
Zhang et al (2017) Protein kinase D at the Golgi controls NLRP3 inflammasome activation. J Exp Med 214 2671 PMID: 28716882
Xu et al (2015) GPCR-mediated PLCβγ/PKCβ/PKD signaling pathway regulates the cofilin phosphatase slingshot 2 in neutrophil chemotaxis. Biochem Biophys Res Commun 26 874 PMID: 25568344
Zheng et al (2011) Ligand-stimulated downregulation of the alpha IF. receptor: role of protein kinase D2. Mol Cell Biol 31 710 PMID: 21173164
Dokas et al (2011) Multiple protein kinases determine the phosphorylated state of the small heat shock protein, HSP27, in SH-SY5Y neuroblastoma cells. Neuropharmacology 61 12 PMID: 21338617
Chen and Kan (2015) Down-regulation of superoxide dismutase 1 by PMA is involved in cell fate determination and mediated via protein kinase D2 in myeloid leukemia cells. Biochim Biophys Acta 1853 2662 PMID: 26241492
Torres-Marquez et al (2010) CID755673 enhances mitogenic signaling by phorbol esters, bombesin and EGF through a protein kinase D-independent pathway. J Biol Chem 391 63 PMID: 19896460
Rezaee et al (2013) Sustained protein kinase D activation mediates respiratory syncytial virus-induced airway barrier disruption. J Virol 87 11088 PMID: 23926335
Kienzle et al (2013) PKD controls mitotic Golgi complex fragmentation through a Raf-MEK1 pathway. Mol Biol Cell 24 222 PMID: 23242995
Spratley et al (2011) Protein kinase D regulates cofilin activity through p21-activated kinase 4. Sci Signal 286 34254 PMID: 21832093
Do you know of a great paper that uses CID 755673 from Tocris? Please let us know.
Reviews for CID 755673
Average Rating: 5 (Based on 1 Review.)
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Effect of CID 755673 on PKD has been under observation..
By
Anonymous on 01/16/2020
Species: Human
Effect of CID 755673 on PKD has been under observation. Changes in the FRET ratio from COS-7 cells expressing the kinase activity reporter, DKAR, following activation of endogenous PKD (light blue diamonds) or overexpressed PKD (dark blue diamonds) via 200 nM PDBu treatment and subsequent PKD inhibition with the non-competitive CID 755673 (50 μM).
