Kenpaullone | GSK-3ß/CDK/KLF4 inhibitor

CAS:
142273-20-9
Catalog Number:
10-3028
Activity:
GSK-3ß/CDK/KLF4 inhibitor
Chemical Names:
9-Bromo-7,12-dihydro-indolo[3,2-d]benzazepine-6(5H)-one; NSC 664704
Molecular Weight:
327.18
Molecular Formula:
C16H11BrN2O
Solubility:
Soluble in DMSO (35 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$80.00
25 mg$240.00

Kenpaullone (142273-20-9) inhibits GSK-3β (IC50=0.23 µM) as well as several cyclin-dependent kinases (CDKs), IC50=0.4, 0.68 and 0.85 µM for cdk1, cdk2 and cdk5 respectively.1-3 Induces pluripotent stem cells from somatic cells4 and increases direct neural conversion of human fibroblasts5 when used with other small molecules. Inhibits Kruppel-Like Factor 4 (KLF4) reducing autoimmune arthritis in the collagen-induced arthritis mouse model.6

References/Citations:

  1. Zaharevitz et al. (1999), Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases; Cancer Res. 59 2566
  2. Schultz et al. (1999) Paullones, a series of cyclin-dependent kinase inhibitor: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity; J.Med.Chem. 42 2909
  3. Bain et al. (2003), The specificities of protein kinase inhibitors: an update; J. 371(Pt. 1) 199
  4. Lyssiotis et al. (2009) Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4; Natl. Acad. Sci. USA 106 8912
  5. Pfisterer et al. (2016), Small molecules increase direct neural conversion of human fibroblasts; Rep. 6 38290
  6. Choi et al. (2018), Kruppel-Like Factor 4 Positively Regulates Autoimmune Arthritis in Mouse Models and Rheumatoid Arthritis in Patients via Modulating Cell Survival and Inflammation Factors of Fibroblast-Like Synoviocyte; Immunol. 9 1339
CAS:
142273-20-9
Catalog Number:
10-3028
Activity:
GSK-3ß/CDK/KLF4 inhibitor
Chemical Names:
9-Bromo-7,12-dihydro-indolo[3,2-d]benzazepine-6(5H)-one; NSC 664704
Molecular Weight:
327.18
Molecular Formula:
C16H11BrN2O
Solubility:
Soluble in DMSO (35 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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