All Photos(1)
Synonym(s):
9-Bromo-7,12-dihydro-indolo[3,2-d][1]benzazepin-6(5H)-one, NSC 664704
Empirical Formula (Hill Notation):
C16H11BrN2O
CAS Number:
Molecular Weight:
327.18
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥98%
form
solid
color
yellow
solubility
DMSO: 18 mg/mL, clear, yellow
storage temp.
2-8°C
SMILES string
Brc1ccc2[nH]c-3c(CC(=O)Nc4ccccc-34)c2c1
InChI
1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)
InChI key
QQUXFYAWXPMDOE-UHFFFAOYSA-N
Gene Information
human ... CDC2(983)
mouse ... Gsk3b(56637)
rat ... Gsk3b(84027)
Application
Kenpaullone has been used:
- as a glycogen synthase kinase 3 (GSK3)/ cyclin-dependent kinase (CDK) inhibitor to study its effects on human neural progenitor cell lines
- as an inhibitor of Krupple-like factor 4 (KLF4) in Gs-coupled designer GPCR (Gs DREADD= GsD) Agouti-related peptide (GsD-AgRP) mice
- as a GSK3/CDK inhibitor to study its effects on the sea urchin embryo development
Biochem/physiol Actions
Kenpaullone is also an inhibitor of glycogen synthase kinase 3β (GSK3β). It also inhibits cyclin-dependent kinase 1 (CDK1/cyclin B), CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25, majorly by competitive inhibition of adenosine triphosphate (ATP) binding.
Features and Benefits
This compound is featured on the CDKs and GSK-3 pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Packaging
Store under argon
WGK
WGK 3
Personal Protective Equipment
dust mask type N95 (US), Eyeshields, Gloves
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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D W Zaharevitz et al.
Cancer research, 59(11), 2566-2569 (1999-06-11)
Analysis of the National Cancer Institute Human Tumor Cell Line Anti-Cancer Drug Screen data using the COMPARE algorithm to detect similarities in the pattern of compound action to flavopiridol, a known inhibitor of cyclin-dependent kinases (CDKs), has suggested several possible
Tomohiro Kitabayashi et al.
Scientific reports, 9(1), 10049-10049 (2019-07-13)
Cancer stem cells are associated with chemoresistance and rapid recurrence of malignant tumors, including glioblastoma (GBM). Although temozolomide (TMZ) is the most effective drug treatment for GBM, GBM cells acquire resistance and become refractory to TMZ during treatment. Therefore, glioma
Ken-ichiro Nakajima et al.
Nature communications, 7, 10268-10268 (2016-01-09)
Agouti-related peptide (AgRP) neurons of the hypothalamus play a key role in regulating food intake and body weight, by releasing three different orexigenic molecules: AgRP; GABA; and neuropeptide Y. AgRP neurons express various G protein-coupled receptors (GPCRs) with different coupling
Letizia Anello et al.
Comparative biochemistry and physiology. Toxicology & pharmacology : CBP, 204, 36-44 (2017-11-13)
The selection and validation of bioactive compounds require multiple approaches, including in-depth analyses of their biological activity in a whole-animal context. We exploited the sea urchin embryo in a rapid, medium-scale range screening to test the effects of the small
AZD5438 a GSK-3a/b and CDK inhibitor is antiapoptotic modulates mitochondrial activity and protects human neurons from mitochondrial toxins.
Shi, et al.
Scientific Reports, 13, 8334-8334 (2023)
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