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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
5 mg | $70 | In Stock | |
10 mg | $101 | In Stock | |
25 mg | $197 | In Stock | |
50 mg | $358 | In Stock | |
100 mg | $511 | In Stock | |
200 mg | $692 | In Stock | |
1 mL x 10 mM (in DMSO) | $68 | In Stock |
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 | CDK8:0.83 μM, CDK19:0.31 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 |
Smiles | N#Cc1ccc2ncnc(NCCc3ccccc3)c2c1 |
Relative Density. | 1.24 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (364.54 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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