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Merck

K3888

Kenpaullone

≥98%

동의어(들):

9-Bromo-7,12-dihydro-indolo­[3,2-d]­[1]benzazepin-6(5H)-one, NSC 664704

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C16H11BrN2O
CAS 번호:
Molecular Weight:
327.18
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98%
Form:
solid
Quality level:
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InChI key

QQUXFYAWXPMDOE-UHFFFAOYSA-N

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)

assay

≥98%

form

solid

color

yellow

solubility

DMSO: 18 mg/mL, clear, yellow

storage temp.

2-8°C

Quality Level

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

저장 등급

11 - Combustible Solids

wgk

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves


가장 최신 버전 중 하나를 선택하세요:

시험 성적서(COA)

Lot/Batch Number

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문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

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
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
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
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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