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CID755673

Cat. No. M3747

CID755673 Structure
Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 125 In stock
50mg USD 380 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CID755673 suppressed half of the PKD1 enzyme activity at 182 nm and exhibited selective PKD1 inhibition when compared with AKT, polo-like kinase 1 (PLK1), CDK activating kinase (CAK), CAMKIIalpha, and three different PKC isoforms.In cell-based assays, CID755673 blocked phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. Functionally, CID755673 inhibited the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. Moreover, CID755673 inhibited prostate cancer cell proliferation, cell migration, and invasion. Treatment with CK59 and CID755673 indeed resulted in a significant dose-dependent reduction of NK cell degranulation markers and cytokine release in freshly isolated Peripheral blood mononuclear cell populations from healthy blood donors.

Protocol
Cell Experiment
Cell lines LNCaP or PC3 cells
Preparation method Counting the number of viable cells upon trypan blue staining to determine cell proliferation . Using cellTiter-Glo Luminescent Cell Viability Assay to measure Cell proliferation by according to the manufacturer's instructions.
Concentrations ~25 μM
Incubation time 6 days
Animal Experiment
Animal models Rat pancreatitis model
Formulation DMSO
Dosages ~15 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 217.22
Formula C12H11NO3
CAS Number 521937-07-5
Purity >99%
Solubility DMSO
Storage at -20°C
References

Protein Kinase Inhibitors CK59 and CID755673 Alter Primary Human NK Cell Effector Functions.
Scheiter M, et al. Front Immunol. 2013 Mar 18;4:66. PMID: 23508354.

Protein kinase D promotes in vitro osteoclast differentiation and fusion.
Mansky KC, et al. J Biol Chem. 2013 Apr 5;288(14):9826-34. PMID: 23430742.

CID755673 enhances mitogenic signaling by phorbol esters, bombesin and EGF through a protein kinase D-independent pathway.
Torres-Marquez E, et al. Biochem Biophys Res Commun. 2010 Jan 1;391(1):63-8. PMID: 19896460.

Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone.
Sharlow ER, et al. J Biol Chem. 2008 Nov 28;283(48):33516-26. PMID: 18829454.

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CID-2011756 is a cell-active ATP competitive and specific PKD1 inhibitor that inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CID755673 supplier, PKD, inhibitors

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