| Name | Senexin A |
| 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. |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (14.58 mM), Sonication is recommended.
DMSO : 100 mg/mL (364.54 mM), Sonication is recommended.
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| Keywords | Senexin A | Inhibitor | inhibit | Cyclin dependent kinase | CDK8 | CDK |
| Inhibitors Related | Ribociclib | (E)-β-Farnesene | Amantadine | 2-Chloropyrazine | Kojic acid | Abemaciclib | 2,4,6-Trihydroxybenzoic acid | Palbociclib | Abemaciclib methanesulfonate | Sodium Oxamate | Seliciclib | Dinaciclib |
| Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | High-Efficiency Gene Editing Small Molecule Library |
United States
