Senexin A

Modify Date: 2024-01-01 17:16:24

Senexin A Structure
Senexin A structure
Common Name Senexin A
CAS Number 1366002-50-7 Molecular Weight 274.32000
Density N/A Boiling Point N/A
Molecular Formula C17H14N4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Senexin A


Senexin A is a CDK8 inhibitor with an IC50 of 280 nM.

 Names

Name 4-(Phenethylamino)quinazoline-6-carbonitrile
Synonym More Synonyms

 Senexin A Biological Activity

Description Senexin A is a CDK8 inhibitor with an IC50 of 280 nM.
Related Catalog
Target

CDK19:0.31 μM (Kd)

CDK8:0.83 μM (Kd)

In Vitro 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. The induction of transcription factor EGR1 upon serum starvation, followed by readdition of serum, is strongly inhibited by Senexin A in HT1080 cells. Senexin A inhibits only p21-induced transcription but not other biological effects of p21. Senexin A also decreases the expression of many secreted tumor-promoting factors in doxorubicin-treated wild-type HCT116 cells[1].
In Vivo Five daily treatment of Senexin A fully reverses tumor-promoting effect of chemotherapy. Senexin A shows no detectable toxicity and no significant effects on body weight, organ weights, or blood cell counts in C57BL/6 mice during the treatment. This effect of doxorubicin treatment is completely abolished, however, when doxorubicin injection is followed by administration of Senexin A. Senexin A treatment strongly improves the response of A549/MEF tumors to doxorubicin[1].
Animal Admin Mice: Senexin A toxicity study is conducted by Taconic in C57BL/6 mice, using five mice per group treated with 20 mg/kg Senexin A or carrier (80% propylene glycol), with five daily i.p. injections. Mice are weighed on days 3 and 6, and killed on day 6. Organ weights are determined for brain, kidney, thymus, spleen, lung, and liver. Terminal blood samples are analyzed to determine the numbers of total white blood cells, neutrophils, lymphocytes, monocytes, eosinophils, and basophils[1].
References

[1]. Porter DC, et al. Cyclin-dependent kinase 8 mediates chemotherapy-induced tumor-promoting paracrine activities. Proc Natl Acad Sci U S A. 2012 Aug 21;109(34):13799-804.

 Chemical & Physical Properties

Molecular Formula C17H14N4
Molecular Weight 274.32000
Exact Mass 274.12200
PSA 61.60000
LogP 3.22908
Storage condition -20℃

 Synonyms

Senexin A
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