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kb-NB142-70

Cat. No. M8382
kb-NB142-70 Structure
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Quality Control & Documentation
Biological Activity

kb-NB142-70 is a derivative of the PKD1 inhibitor CID755673, with approximately 6-fold greater potency (IC50 for inhibition of PKD1 = 28.3 nM vs. 182 nM for CID755673). kb-NB142-70 dose dependently inhibits proliferation of PC3 prostate cancer cell, and blocks migration of the prostate cancer lines PC3 and DU145.

Chemical Information
Molecular Weight 251.32
Formula C11H9NO2S2
CAS Number 1233533-04-4
Solubility (25°C) DMSO: 10 mg/mL
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] Jia Wang, et al. Biphasic Regulation of Yes-associated Protein (YAP) Cellular Localization, Phosphorylation, and Activity by G Protein-coupled Receptor Agonists in Intestinal Epithelial Cells: A NOVEL ROLE FOR PROTEIN KINASE D (PKD)

[2] Ning Wei, et al. Protein kinase d as a potential chemotherapeutic target for colorectal cancer

[3] Jianxia Guo, et al. In vitro cytotoxicity, pharmacokinetics, tissue distribution, and metabolism of small-molecule protein kinase D inhibitors, kb-NB142-70 and kb-NB165-09, in mice bearing human cancer xenografts

[4] Karla Bravo-Altamirano, et al. Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D

[5] Courtney R Lavalle, et al. Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility

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  Catalog
Abmole Inhibitor Catalog




Keywords: kb-NB142-70 supplier, inhibitors, activators


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