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CID755673

Cat. No. M3747
CID755673 Structure
Size Price Availability Quantity
5mg USD 65  USD65 In stock
10mg USD 95  USD95 In stock
50mg USD 265  USD265 In stock
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Quality Control & Documentation
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 (for reference only)
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.
Chemical Information
Molecular Weight 217.22
Formula C12H11NO3
CAS Number 521937-07-5
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Scheiter M, et al. Front Immunol. Protein Kinase Inhibitors CK59 and CID755673 Alter Primary Human NK Cell Effector Functions.

[2] Mansky KC, et al. J Biol Chem. Protein kinase D promotes in vitro osteoclast differentiation and fusion.

[3] Torres-Marquez E, et al. Biochem Biophys Res Commun. CID755673 enhances mitogenic signaling by phorbol esters, bombesin and EGF through a protein kinase D-independent pathway.

[4] Sharlow ER, et al. J Biol Chem. Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone.

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Keywords: CID755673 supplier, PKD, inhibitors, activators


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