Home Cell Cycle CDK inhibitor Senexin A For research use only.

Senexin A

Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively.

Senexin A Chemical Structure

Senexin A Chemical Structure

CAS: 1366002-50-7

Selleck's Senexin A has been cited by 2 publications

Purity & Quality Control

Batch: S852001 DMSO] 54 mg/mL] false] Ethanol] 54 mg/mL] false] Water] Insoluble] false Purity: 99.89%
99.89

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Biological Activity

Description Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively.
Targets
CDK19 [1]
(Cell-free assay)		 CDK8 [1]
(Cell-free assay)
0.31 μM(Kd) 0.83 μM(Kd)
In vitro
In vitro p21 is shown to activate NF-κB–dependent transcription, and Senexin A inhibits p21-stimulated activity of the consensus NF-κB–dependent promoter. Senexin A has no effect on p21 induction by IPTG, on cell growth with or without p21, or on p21-induced senescent phenotype. Senexin A does not affect the inhibition of gene expression by p21 and does not interfere with p21-mediated inhibition of large sets of genes belonging to Gene Ontology (GO) categories of mitosis and DNA replication. Senexin A inhibits only p21-induced transcription but not other biological effects of p21. Senexin A inhibits CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively and CDK8 kinase activity with IC50 of 0.28 μM. Senexin A inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells. It does not inhibit ROCK and did not share cortistatin A's strong antiendothelial cell activity[1].
Cell Research Cell lines MEF
Concentrations 1 μM
Incubation Time 24 h
Method

For conditioned media mitogenic assays, MEF, untreated or treated for 24 h with 200 nM doxorubicin, alone or in combination with 1 μM Senexin A, were washed and cultured for 48 h without drugs to collect conditioned media. The media were added to A549 cells, plated on 12-well plates at 104 cells per well; cells were counted after 48 h using the trypan blue exclusion assay. Experiments were performed in triplicate, and cells counted in at least three optical fields per experiment.
Experimental Result Images Methods Biomarkers Images PMID
Western blot GLUT1 / GLUT3 / HK1 / HIF1A / CDK8 29117556
In Vivo
In vivo The CDK8/19 inhibitor Senexin A reverses chemotherapy-induced paracrine tumor-promoting activities in vivo and does not inhibit reporter cell growth and showed no detectable toxicity in a mouse study[1].
Animal Research Animal Models C57BL/6 mice
Dosages 20 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 274.32 Formula

C17H14N4
CAS No. 1366002-50-7 SDF Download Senexin A SDF
Smiles C1=CC=C(C=C1)CCNC2=NC=NC3=C2C=C(C=C3)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (196.85 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 54 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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