Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&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. |
動物実験 | 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. |
分子量 | 274.32 |
分子式 | C17H14N4 |
CAS No. | 1366002-50-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (364.54 mM)
You can also refer to dose conversion for different animals. 詳細
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Senexin A 1366002-50-7 Cell Cycle/Checkpoint CDK Cyclin dependent kinase Inhibitor inhibit inhibitor