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Senexin A

Catalog No. T5673   CAS 1366002-50-7

Senexin A is an effective and selective CDK8 inhibitor that also inhibits CDK19 with Kd values of 0.83 microns and 0.31 microns, respectively.

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Senexin A Chemical Structure
Senexin A, CAS 1366002-50-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
2 mg In stock $ 72.00
5 mg In stock $ 116.00
10 mg In stock $ 168.00
25 mg In stock $ 328.00
50 mg In stock $ 597.00
100 mg In stock $ 852.00
1 mL * 10 mM (in DMSO) In stock $ 113.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Senexin A is an effective and selective CDK8 inhibitor that also inhibits CDK19 with Kd values of 0.83 microns and 0.31 microns, respectively.
Targets&IC50 CDK19:0.31 μm, CDK8:0.83 μM
In vitro Senexin A inhibited 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.CDK8 stimulates Wnt/β-catenin, and Senexin A inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells.
In vivo Administering Senexin A daily for five days completely counteracts the tumor-promoting effects of chemotherapy, displaying no detectable toxicity or significant impacts on body weight, organ weights, or blood cell counts in C57BL/6 mice. The adverse effects of doxorubicin treatment are entirely negated when followed by Senexin A administration, significantly enhancing the responsiveness of A549/MEF tumors to doxorubicin.
Animal Research Tumor-free C57BL/6-derived SCID mice were injected with a single dose of doxorubicin or carrier control.?Five days later, mice received. injection of 2 × 10^6 human A549 lung carcinoma cells, and tumor take was measured over 4 wk.
Molecular Weight 274.32
Formula C17H14N4
CAS No. 1366002-50-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (364.54 mM)

TargetMolReferences and Literature

1. Porter D C , Farmaki E , Altilia S , et al. Cyclin-dependent kinase 8 mediates chemotherapy-induced tumor-promoting paracrine activities[J]. Proceedings of the National Academy of Sciences, 2012, 109(34):13799-13804.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Cell Cycle Compound Library Kinase Inhibitor Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library NO PAINS Compound Library Bioactive Compound Library Anti-Aging Compound Library

Related Products

Related compounds with same targets
Palbociclib monohydrochloride Flavopiridol JSH-150 THZ1-R CGP60474 Voruciclib HQ461 CDK2-IN-4

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Keywords

Senexin A 1366002-50-7 Cell Cycle/Checkpoint CDK Cyclin dependent kinase Inhibitor inhibit inhibitor

 

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