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Kenpaullone

Cat. No. M3774
Kenpaullone Structure
Synonym:

NSC-664704, 9-Bromopaullone, 9-Bromo-7

Size Price Availability Quantity
10mg USD 115  USD115 In stock
25mg USD 245  USD245 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

Kenpaullone represents a novel chemotype for compounds that preferentially inhibit CDKs. Kenpaullone inhibits CDK2/cyclin A, CDK2/cyclin E and CDK5/cyclin/p35 (IC50 values are 0.68, 7.5 and 0.85 μM respectively). Kenpaullone is selective over c-src (IC50 = 15 μM), casein kinase 2 (IC50 = 20 μM), ERK1 (IC50 = 20 μM), ERK2 (IC50 = 9 μM) and a range of other protein kinases (IC50 values > 35 μM). Kenpaullone generates induced pluripotent stem cells (iPSCs) from somatic cells when used in combination with reprogramming factors. Kenpaullone can take the place of Klf4.

Protocol (for reference only)
Cell Experiment
Cell lines HEK-293 cells
Preparation method
Concentrations 10μM
Incubation time 0-12h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 327.18
Formula C16H11BrN2O
CAS Number 142273-20-9
Solubility (25°C) DMSO 18 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] Lyssiotis CA, et al. Proc Natl Acad Sci U S A. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4.v

[2] Buolamwini JK. Curr Pharm Des. Cell cycle molecular targets in novel anticancer drug discovery.

[3] Schultz C, et al. J Med Chem. Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.

[4] Zaharevitz DW, et al. Cancer Res. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases.

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Keywords: Kenpaullone, NSC-664704, 9-Bromopaullone, 9-Bromo-7 supplier, CDK, inhibitors, activators


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