Free shipping on all orders over $ 500

Kenpaullone

Cat. No. M3774

Kenpaullone Structure

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

Size Price Availability Quantity
10mg USD 110 In stock
50mg USD 380 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
Cell Experiment
Cell lines HEK-293 cells
Preparation method
Concentrations 10μM
Incubation time 0-12h
Animal Experiment
Animal models
Formulation
Dosages
Administration
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 327.18
Formula C16H11BrN2O
CAS Number 142273-20-9
Purity >99%
Solubility DMSO 18 mg/mL
Storage at -20°C
References

Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4.v
Lyssiotis CA, et al. Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7. PMID: 19447925.

Cell cycle molecular targets in novel anticancer drug discovery.
Buolamwini JK. Curr Pharm Des. 2000 Mar;6(4):379-92. PMID: 10788588.

Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.
Schultz C, et al. J Med Chem. 1999 Jul 29;42(15):2909-19. PMID: 10425100.

Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases.
Zaharevitz DW, et al. Cancer Res. 1999 Jun 1;59(11):2566-9. PMID: 10363974.

Related CDK Products
NU2058

NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.

LDC000067

LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.

RO-3306

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

LDC4297

LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs).

THZ1

THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.